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Entinostat (MS-275)

別名: SNDX-275 中文名稱：恩替諾特

Entinostat (MS-275, SNDX-275)強(qiáng)烈抑制HDAC1和HDAC3，無細(xì)胞試驗(yàn)中IC50分別為0.51 μM和1.7 μM，抑制作用強(qiáng)于HDACs 4， 6， 8，和10。Entinostat可誘導(dǎo)自噬和凋亡。Phase 3。

Entinostat (MS-275) Chemical Structure

Entinostat (MS-275) Chemical Structure

CAS: 209783-80-2

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 746.45 現(xiàn)貨
10mg 794.43 現(xiàn)貨
50mg 2234.07 現(xiàn)貨
200mg 4668.3 現(xiàn)貨
1g 7944.3 現(xiàn)貨
更大包裝 有超大折扣

400-668-6834

info@selleck.cn
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常與Entinostat (MS-275)一起在實(shí)驗(yàn)中被使用的化合物

Vorinostat (SAHA)

Entinostat和Vorinostat證明了潛伏感染的原代T細(xì)胞中激活了HIV的產(chǎn)生。

Wightman F, et al. AIDS. 2013 Nov 28; 27(18): 2853–2862.

Panobinostat (LBH589)

Entinostat和Panobinostat可以下調(diào)HR熟練的人卵巢癌細(xì)胞中選定HR基因的表達(dá)。

Quisinostat (JNJ-26481585) 2HCl

Entinostat和Quisinostat 2HCl是HDAC抑制劑，可預(yù)防CaMKII過度表達(dá)誘導(dǎo)的心肌細(xì)胞肥大。

Zhang M, et al. J Mol Cell Cardiol. 2020 Dec;149:73-81.

Exemestane

Entinostat和Exemestane可顯著改善晚期激素受體陽性、HER2陰性乳腺癌的無進(jìn)展生存期和總生存期。

Connolly RM, et al. J Clin Oncol. 2021 Oct 1;39(28):3171-3181.

Decitabine

Entinostat和Decitabine誘導(dǎo)J82、J82CisR和RT-112細(xì)胞凋亡，并誘導(dǎo)J82和RT-112細(xì)胞系細(xì)胞周期停滯。

Wang C, et al. Cancers (Basel). 2020 Feb 3;12(2):337.

Entinostat (MS-275)相關(guān)產(chǎn)品

相關(guān)信號通路圖

HDAC Signaling Pathways

HDAC信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
U937 Function assay 5 uM 24 hrs Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis. 17447750
HCT116 Function assay 10 uM 24 hrs Inhibition of HDAC1 in human HCT116 cells assessed as induction of hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. 20452226
NB4 Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis. 20491440
NB4 Function assay 5 uM 24 hrs Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis. 20491440
epithelial cells Function assay 1 uM 4, 6, and 8 days Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in short circuit currents at 1 uM for 4, 6, and 8 days relative to control. 19966789
Hela Function assay 0.6 uM 16 hrs Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy. 21696956
U937 Cell cycle arrest assay 5 uM 30 hrs Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry. 21215647
NB4 Function assay 5 uM 24 hrs Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis. 20491440
C127-LT Function assay 1 uM 24 hrs Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 1 uM after 24 hrs by fluorescence microscopy. 26996372
C127-LT Function assay 10 uM 24 hrs Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy. 26996372
HCT116 Function assay 10 uM 24 hrs Inhibition of HDAC2 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. 22321215
HCT116 Function assay 10 uM 24 hrs Inhibition of HDAC1 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. 22321215
HeLa Function assay 1 uM 6 hrs Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 1 uM after 6 hrs by Western blot analysis. 29787262
MV4-11 Apoptosis assay 5 uM 24 to 48 hrs Induction of apoptosis in human MV4-11 cells at 5 uM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry. 29738953
MV4-11 Function assay 200 nM 24 hrs Inhibition of class 1 HDAC in human MV4-11 cells assessed as hyperacetylation of histone H3 at 200 nM after 24 hrs by Western blot analysis. 29738953
HL60 Apoptosis assay 5 uM 48 hrs Induction of apoptosis in human HL60 cells assessed as decrease in procaspase-3 level at 5 uM after 48 hrs by Western blot analysis. 28415009
HL60 Apoptosis assay 5 uM 48 hrs Induction of apoptosis in human HL60 cells assessed as increase in cleaved caspase-3 level at 5 uM after 48 hrs by Western blot analysis. 28415009
HL60 Apoptosis assay 5 uM 48 hrs Induction of apoptosis in human HL60 cells assessed as increase in cleaved PARP level at 5 uM after 48 hrs by Western blot analysis. 28415009
MV4-11 Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. 29589441
HEL Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human HEL cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. 29589441
Jurkat Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human Jurkat cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. 29589441
MV4-11 Function assay 5 uM 24 hrs Inhibition of class 1 HDAC in human MV4-11 cells assessed as induction of histone hyperacetylation at 5 uM after 24 hrs by Western blot method. 29589441
LNCAP Function assay 10 uM 24 hrs Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation at 10 uM measured after 24 hrs relative to control. 27717544
epithelial cells Function assay 5 uM Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM. 19966789
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 22705022
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 22705022
SK-N-BE(2) Antiproliferative assay 48 hrs Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.33 μM. 28511906
AGS Antiproliferative assay 72 hrs Antiproliferative activity against human AGS cells after 72 hrs by MTT assay, IC50 = 0.34 μM. 29787262
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay, IC50 = 0.35 μM. 26613635
HEL Function assay 3 hrs Inhibition of class 1 HDAC in HEL cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.43 μM. 28511906
PC3 Growth inhibition assay 48 hrs Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay, GI50 = 0.43 μM. 28395150
HEL Antiproliferative assay 72 hrs Antiproliferative activity against human HEL cells after 72 hrs by MTT assay, IC50 = 0.44 μM. 29787262
MOLT4 Antiproliferative assay 72 hrs Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay, IC50 = 0.45 μM. 29787262
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay, IC50 = 0.47 μM. 29202397
HEL Antiproliferative assay 48 hrs Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 0.48 μM. 28511906
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay, IC50 = 0.55 μM. 25953722
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.55 μM. 25874326
HCT116 Growth inhibition assay 2 days Growth inhibition of human HCT116 cells after 2 days by MTT assay, GI50 = 0.6 μM. 22541394
HL60 Function assay 3 hrs Inhibition of class 1 HDAC in human HL60 cells using Boc-Ac-Lys-AMC as substrate incubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.62 μM. 28415009
MOLT4 Antiproliferative assay 48 hrs Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.65 μM. 28511906
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 0.7 μM. 19441846
HEK293T Function assay 1 hr Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 0.74 μM. 29289885
HCT116 Antiproliferative assay 3 days Antiproliferative activity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.76 μM. 22321215
U937 Antiproliferative assay 48 hrs Antiproliferative activity against human U937 cells after 48 hrs by MTT assay, IC50 = 0.77 μM. 28415009
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.78 μM. 25874326
K562 Function assay 10 mins Inhibition of KDAC3 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 0.79 μM. 26681404
HCT116 Cytotoxicity assay 3 days Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.8 μM. 20452226
Sf9 Function assay 3 hrs Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method, IC50 = 0.9 μM. 28501514
HEK293T Function assay 1 hr Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.07 μM. 29289885
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.2 μM. 19441846
HEK293T Function assay 1 hr Inhibition of human FLAG-tagged HDAC3 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.23 μM. 29289885
HEL Antiproliferative assay 48 hrs Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 1.29 μM. 28415009
G401 Antiproliferative assay 72 hrs Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.3 μM. 19441846
Sf9 Function assay 3 hrs Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM SAHA by f, IC50 = 1.3 μM. 28501514
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.32 μM. 28511906
Huh7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 1.4 μM. 25490700
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.41 μM. 28395150
K562 Function assay 10 mins Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 1.48 μM. 26681404
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 1.52 μM. 28415009
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay, IC50 = 1.6 μM. 29202397
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.68 μM. 28415009
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.8 μM. 19441846
HCT116 Function assay 18 hrs Inhibition of HDAC in human HCT116 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 1.96 μM. 28340413
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.03 μM. 28340413
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.07 μM. 28415009
NCI-H661 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 2.19 μM. 25874326
NCI-H661 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay, IC50 = 2.19 μM. 25953722
Sf9 Function assay 17 hrs Inhibition of His6-tagged HDAC3/SMRT (395 to 489 residues) (unknown origin) co-expressed in baculovirus infected sf9 cells using (FAM)-labeled acetylated peptide substrate after 17 hrs by caliper microfluidic mobility shift assay, IC50 = 2.31206 μM. 30179749
ACHN Antiproliferative assay 72 hrs Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2.4 μM. 29787262
SGC7901 Growth inhibition assay 72 hrs Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 2.5 μM. 23061376
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 2.55 μM. 29787262
MDA-MB-231 Anticancer assay 72 hrs Anticancer activity against human MDA-MB-231 cells after 72 hrs by MTT assay, GI = 2.8 μM. 21741834
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 3 μM. 19441846
HCT116 Anticancer assay 72 hrs Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, GI = 3.1 μM. 21741834
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 3.1 μM. 29787262
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 3.11 μM. 28340413
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 3.134 μM. 26140961
A2780 Function assay 18 hrs Inhibition of HDAC in human A2780 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 3.15 μM. 28340413
HeLa Function assay 30 mins Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay, IC50 = 3.2 μM. 21889343
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 3.66 μM. 29787262
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay, IC50 = 3.67 μM. 29202397
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 4.02 μM. 28340413
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 4.53 μM. 28340413
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 4.63 μM. 25874326
MGC803 Antiproliferative assay 72 hrs Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay, IC50 = 4.89 μM. 29202397
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 4.89 μM. 28511906
HuH7 Cytotoxicity assay 3 days Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 5.1 μM. 25490700
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 5.1 μM. 26140961
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 5.41 μM. 25874326
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay, IC50 = 5.41 μM. 25953722
A2780 Anticancer assay 72 hrs Anticancer activity against human A2780 cells after 72 hrs by MTT assay, GI = 5.7 μM. 21741834
A549 Growth inhibition assay 48 hrs Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay, GI50 = 5.76 μM. 28395150
A2780 Antiproliferative assay 48 hrs Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay, IC50 = 5.89 μM. 28340413
SMMC7721 Antiproliferative assay 72 hrs Antiproliferative activity against human SMMC7721 cells after 72 hrs by CCK-8 assay, IC50 = 5.97 μM. 29202397
U266 Antiproliferative assay 48 hrs Antiproliferative activity against human U266 cells after 48 hrs by MTT assay, IC50 = 6.1 μM. 28415009
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 6.36 μM. 28340413
U251 Growth inhibition assay 2 days Growth inhibition of human U251 cells after 2 days by MTT assay, GI50 = 6.5 μM. 22541394
NCI-H1299 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay, IC50 = 6.74 μM. 29202397
AsPC1 Growth inhibition assay 48 hrs Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay, GI50 = 6.9 μM. 28395150
BGC823 Growth inhibition assay 72 hrs Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 7.1 μM. 23061376
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 7.881 μM. 26140961
DU145 Anticancer assay 72 hrs Anticancer activity against human DU145 cells after 72 hrs by MTT assay, GI = 7.9 μM. 21741834
Bel7402 Growth inhibition assay 72 hrs Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8 μM. 23061376
HeLa Function assay 20 mins Inhibition of HDAC in human HeLa cells using fluor de Lys as substrate incubated for 20 mins by microplate spectrofluorometric analysis, IC50 = 8.02 μM. 27060764
MGC803 Growth inhibition assay 72 hrs Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8.9 μM. 23061376
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, GI50 = 9.32 μM. 28629630
SMMC7721 Growth inhibition assay 72 hrs Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 11 μM. 23061376
HeLa Function assay 24 to 48 hrs Inhibition of HDAC in human HeLa cells using Boc-Lys(AC)-AMC as substrate after 24 to 48 hrs by spectrofluorometry, IC50 = 11.18 μM. 26996372
SKHEP1 Growth inhibition assay 72 hrs Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 13 μM. 23061376
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50 = 18.37 μM. 28629630
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, GI50 = 19.09 μM. 28629630
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50 = 19.24 μM. 28629630
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, GI50 = 19.26 μM. 28629630
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 27.47 μM. 18701301
U251 Growth inhibition assay 2 days Growth inhibition of human U251 cells after 2 days by MTT assay, TGI = 40 μM. 22541394
HEK293 STF Function assay 24 hrs Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay. 19022675
A4-Fuk Growth Inhibition Assay IC50=1.15364 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=1.13165 μM SANGER
LC-1F Growth Inhibition Assay IC50=1.12007 μM SANGER
PF-382 Growth Inhibition Assay IC50=1.11513 μM SANGER
L-540 Growth Inhibition Assay IC50=1.10604 μM SANGER
TGW Growth Inhibition Assay IC50=1.07675 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=1.03454 μM SANGER
SH-4 Growth Inhibition Assay IC50=1.0241 μM SANGER
HH Growth Inhibition Assay IC50=0.98959 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=0.97831 μM SANGER
DMS-153 Growth Inhibition Assay IC50=0.97469 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.9683 μM SANGER
ES6 Growth Inhibition Assay IC50=0.96437 μM SANGER
LXF-289 Growth Inhibition Assay IC50=0.95901 μM SANGER
GOTO Growth Inhibition Assay IC50=0.95076 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.93284 μM SANGER
EHEB Growth Inhibition Assay IC50=0.92585 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.88687 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.88096 μM SANGER
ST486 Growth Inhibition Assay IC50=0.87917 μM SANGER
JAR Growth Inhibition Assay IC50=0.87827 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.87171 μM SANGER
ES4 Growth Inhibition Assay IC50=0.85868 μM SANGER
BL-70 Growth Inhibition Assay IC50=0.85702 μM SANGER
LC4-1 Growth Inhibition Assay IC50=0.84007 μM SANGER
CESS Growth Inhibition Assay IC50=0.81197 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=0.81084 μM SANGER
CPC-N Growth Inhibition Assay IC50=0.80524 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.80147 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.7836 μM SANGER
BC-3 Growth Inhibition Assay IC50=0.78308 μM SANGER
Daudi Growth Inhibition Assay IC50=0.77681 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.77567 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=0.77348 μM SANGER
SW954 Growth Inhibition Assay IC50=0.75999 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=0.74661 μM SANGER
NB14 Growth Inhibition Assay IC50=0.72617 μM SANGER
COR-L279 Growth Inhibition Assay IC50=0.70996 μM SANGER
KALS-1 Growth Inhibition Assay IC50=0.70492 μM SANGER
ECC12 Growth Inhibition Assay IC50=0.70086 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.68343 μM SANGER
NB13 Growth Inhibition Assay IC50=0.66817 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=0.65947 μM SANGER
CW-2 Growth Inhibition Assay IC50=0.65794 μM SANGER
NALM-6 Growth Inhibition Assay IC50=0.6486 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.64276 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=0.63541 μM SANGER
LOUCY Growth Inhibition Assay IC50=0.63364 μM SANGER
LU-165 Growth Inhibition Assay IC50=0.61812 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=0.60719 μM SANGER
NB69 Growth Inhibition Assay IC50=0.59825 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.58703 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=0.58504 μM SANGER
ONS-76 Growth Inhibition Assay IC50=0.58242 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.57848 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.57073 μM SANGER
BL-41 Growth Inhibition Assay IC50=0.56889 μM SANGER
L-363 Growth Inhibition Assay IC50=0.56657 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=0.56105 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=0.55401 μM SANGER
TE-1 Growth Inhibition Assay IC50=0.55306 μM SANGER
NB17 Growth Inhibition Assay IC50=0.5438 μM SANGER
HL-60 Growth Inhibition Assay IC50=0.54261 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.53663 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.53041 μM SANGER
HCC1599 Growth Inhibition Assay IC50=0.5157 μM SANGER
ACN Growth Inhibition Assay IC50=0.51028 μM SANGER
HC-1 Growth Inhibition Assay IC50=0.50473 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.49661 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=0.49227 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.48358 μM SANGER
K5 Growth Inhibition Assay IC50=0.47025 μM SANGER
LS-513 Growth Inhibition Assay IC50=0.44501 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=0.43897 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=0.43453 μM SANGER
BC-1 Growth Inhibition Assay IC50=0.43403 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=0.43153 μM SANGER
OPM-2 Growth Inhibition Assay IC50=0.41513 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=0.4112 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.41017 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.40613 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.40367 μM SANGER
SCH Growth Inhibition Assay IC50=0.40342 μM SANGER
A101D Growth Inhibition Assay IC50=0.403 μM SANGER
CHP-126 Growth Inhibition Assay IC50=0.40231 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.39868 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=0.38776 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=0.38701 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.38649 μM SANGER
ARH-77 Growth Inhibition Assay IC50=0.38193 μM SANGER
DEL Growth Inhibition Assay IC50=0.37487 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.37121 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.36935 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=0.3673 μM SANGER
ES8 Growth Inhibition Assay IC50=0.36022 μM SANGER
CMK Growth Inhibition Assay IC50=0.35727 μM SANGER
SR Growth Inhibition Assay IC50=0.34261 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.3381 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.33716 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.3351 μM SANGER
NB12 Growth Inhibition Assay IC50=0.31756 μM SANGER
HEL Growth Inhibition Assay IC50=0.31348 μM SANGER
ATN-1 Growth Inhibition Assay IC50=0.30576 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.30256 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.28708 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.27833 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.24079 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.22959 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.20113 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.19619 μM SANGER
SF539 Growth Inhibition Assay IC50=0.19593 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.17627 μM SANGER
CRO-AP2 Growth Inhibition Assay IC50=0.16889 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.13527 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=0.12974 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=0.11579 μM SANGER
ES1 Growth Inhibition Assay IC50=0.11255 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.10912 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=0.10334 μM SANGER
697 Growth Inhibition Assay IC50=0.09976 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.06355 μM SANGER
SCC-3 Growth Inhibition Assay IC50=0.061 μM SANGER
HCC2218 Growth Inhibition Assay IC50=1.16641 μM SANGER
HAL-01 Growth Inhibition Assay IC50=1.16943 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=1.17659 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=1.17898 μM SANGER
EVSA-T Growth Inhibition Assay IC50=1.18114 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.20266 μM SANGER
OCUB-M Growth Inhibition Assay IC50=1.21489 μM SANGER
MEG-01 Growth Inhibition Assay IC50=1.22118 μM SANGER
no-10 Growth Inhibition Assay IC50=1.23112 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=1.24721 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=1.24776 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=1.26478 μM SANGER
CTV-1 Growth Inhibition Assay IC50=1.27425 μM SANGER
NB1 Growth Inhibition Assay IC50=1.27732 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=1.28462 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=1.28577 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=1.28663 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=1.28866 μM SANGER
LP-1 Growth Inhibition Assay IC50=1.29947 μM SANGER
LS-411N Growth Inhibition Assay IC50=1.30998 μM SANGER
CAL-148 Growth Inhibition Assay IC50=1.32542 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=1.34502 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=1.3539 μM SANGER
NCI-H2107 Growth Inhibition Assay IC50=1.35883 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=1.38978 μM SANGER
K-562 Growth Inhibition Assay IC50=1.39219 μM SANGER
PSN1 Growth Inhibition Assay IC50=1.42287 μM SANGER
HCC2157 Growth Inhibition Assay IC50=1.42691 μM SANGER
SBC-1 Growth Inhibition Assay IC50=1.42741 μM SANGER
MC116 Growth Inhibition Assay IC50=1.43615 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=1.45358 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.47103 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=1.47987 μM SANGER
BT-474 Growth Inhibition Assay IC50=1.51764 μM SANGER
A388 Growth Inhibition Assay IC50=1.51945 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=1.5226 μM SANGER
COLO-829 Growth Inhibition Assay IC50=1.53564 μM SANGER
KM-H2 Growth Inhibition Assay IC50=1.5667 μM SANGER
GR-ST Growth Inhibition Assay IC50=1.5682 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=1.60144 μM SANGER
KG-1 Growth Inhibition Assay IC50=1.61901 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=1.63406 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=1.63459 μM SANGER
KM12 Growth Inhibition Assay IC50=1.647 μM SANGER
NB5 Growth Inhibition Assay IC50=1.65677 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=1.68281 μM SANGER
KU812 Growth Inhibition Assay IC50=1.69605 μM SANGER
DB Growth Inhibition Assay IC50=1.70353 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=1.75234 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=1.77207 μM SANGER
ETK-1 Growth Inhibition Assay IC50=1.78879 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=1.79388 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=1.79508 μM SANGER
ES7 Growth Inhibition Assay IC50=1.80302 μM SANGER
SW872 Growth Inhibition Assay IC50=1.81395 μM SANGER
TK10 Growth Inhibition Assay IC50=1.83108 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=1.83563 μM SANGER
TE-9 Growth Inhibition Assay IC50=1.84422 μM SANGER
MLMA Growth Inhibition Assay IC50=1.88234 μM SANGER
D-542MG Growth Inhibition Assay IC50=1.89373 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.9272 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=1.9328 μM SANGER
GB-1 Growth Inhibition Assay IC50=1.93866 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=2.00262 μM SANGER
LAN-6 Growth Inhibition Assay IC50=2.01966 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=2.04502 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=2.05124 μM SANGER
HT Growth Inhibition Assay IC50=2.10454 μM SANGER
RL95-2 Growth Inhibition Assay IC50=2.11482 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=2.11792 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=2.16873 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=2.21723 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=2.26902 μM SANGER
DG-75 Growth Inhibition Assay IC50=2.27148 μM SANGER
ML-2 Growth Inhibition Assay IC50=2.32855 μM SANGER
SF126 Growth Inhibition Assay IC50=2.33094 μM SANGER
MPP-89 Growth Inhibition Assay IC50=2.33145 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=2.33277 μM SANGER
LS-123 Growth Inhibition Assay IC50=2.34936 μM SANGER
NB10 Growth Inhibition Assay IC50=2.41092 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=2.42267 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=2.4777 μM SANGER
L-428 Growth Inhibition Assay IC50=2.48521 μM SANGER
DMS-79 Growth Inhibition Assay IC50=2.54103 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=2.67562 μM SANGER
KGN Growth Inhibition Assay IC50=2.76876 μM SANGER
EW-1 Growth Inhibition Assay IC50=2.77083 μM SANGER
U-266 Growth Inhibition Assay IC50=2.84823 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=2.85641 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=2.87711 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=2.9248 μM SANGER
GI-1 Growth Inhibition Assay IC50=2.92957 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=3.00511 μM SANGER
NCI-H2227 Growth Inhibition Assay IC50=3.02079 μM SANGER
U-87-MG Growth Inhibition Assay IC50=3.03513 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=3.05206 μM SANGER
CTB-1 Growth Inhibition Assay IC50=3.05376 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=3.14378 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=3.16566 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=3.18279 μM SANGER
TE-5 Growth Inhibition Assay IC50=3.21342 μM SANGER
UACC-257 Growth Inhibition Assay IC50=3.43659 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=3.45227 μM SANGER
MFH-ino Growth Inhibition Assay IC50=3.46589 μM SANGER
SF268 Growth Inhibition Assay IC50=3.48174 μM SANGER
TE-12 Growth Inhibition Assay IC50=3.51699 μM SANGER
NB6 Growth Inhibition Assay IC50=3.55563 μM SANGER
DJM-1 Growth Inhibition Assay IC50=3.59899 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=3.61624 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=3.62671 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=3.70947 μM SANGER
RKO Growth Inhibition Assay IC50=3.77189 μM SANGER
ECC4 Growth Inhibition Assay IC50=3.97195 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=3.97547 μM SANGER
EB-3 Growth Inhibition Assay IC50=3.99633 μM SANGER
SHP-77 Growth Inhibition Assay IC50=4.00524 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=4.05625 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=4.06399 μM SANGER
MN-60 Growth Inhibition Assay IC50=4.1087 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=4.13405 μM SANGER
LU-65 Growth Inhibition Assay IC50=4.15332 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=4.18333 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=4.31432 μM SANGER
GT3TKB Growth Inhibition Assay IC50=4.33268 μM SANGER
Becker Growth Inhibition Assay IC50=4.37312 μM SANGER
HCC1187 Growth Inhibition Assay IC50=4.89657 μM SANGER
D-502MG Growth Inhibition Assay IC50=5.00416 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=5.13778 μM SANGER
NB7 Growth Inhibition Assay IC50=5.14112 μM SANGER
SW962 Growth Inhibition Assay IC50=5.38814 μM SANGER
no-11 Growth Inhibition Assay IC50=5.76343 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=5.90694 μM SANGER
COLO-684 Growth Inhibition Assay IC50=5.99494 μM SANGER
D-263MG Growth Inhibition Assay IC50=6.08895 μM SANGER
EW-24 Growth Inhibition Assay IC50=6.2851 μM SANGER
TE-10 Growth Inhibition Assay IC50=6.42623 μM SANGER
EKVX Growth Inhibition Assay IC50=6.46321 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=6.67557 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=6.92301 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=8.13166 μM SANGER
COLO-668 Growth Inhibition Assay IC50=8.27786 μM SANGER
EW-12 Growth Inhibition Assay IC50=8.40803 μM SANGER
A253 Growth Inhibition Assay IC50=8.84661 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=8.89319 μM SANGER
Calu-6 Growth Inhibition Assay IC50=8.99042 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=9.17746 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=9.77478 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=9.97904 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=10.2834 μM SANGER
GCIY Growth Inhibition Assay IC50=10.5924 μM SANGER
TE-15 Growth Inhibition Assay IC50=11.6004 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=11.7682 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=11.7786 μM SANGER
EW-3 Growth Inhibition Assay IC50=12.2463 μM SANGER
CAS-1 Growth Inhibition Assay IC50=12.3631 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=12.6131 μM SANGER
D-247MG Growth Inhibition Assay IC50=12.7952 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=12.8013 μM SANGER
LS-1034 Growth Inhibition Assay IC50=14.3975 μM SANGER
EW-18 Growth Inhibition Assay IC50=14.448 μM SANGER
Raji Growth Inhibition Assay IC50=14.5049 μM SANGER
D-283MED Growth Inhibition Assay IC50=14.6271 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=14.9696 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=15.4633 μM SANGER
P30-OHK Growth Inhibition Assay IC50=17.7831 μM SANGER
RXF393 Growth Inhibition Assay IC50=19.0186 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=20.6703 μM SANGER
U-698-M Growth Inhibition Assay IC50=20.7075 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=20.7223 μM SANGER
SW684 Growth Inhibition Assay IC50=21.1716 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=21.3154 μM SANGER
JVM-2 Growth Inhibition Assay IC50=21.4133 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=22.4148 μM SANGER
CA46 Growth Inhibition Assay IC50=31.6936 μM SANGER
SNB75 Growth Inhibition Assay IC50=33.6503 μM SANGER
KNS-42 Growth Inhibition Assay IC50=35.9624 μM SANGER
TUR Growth Inhibition Assay IC50=36.0521 μM SANGER
REH Growth Inhibition Assay IC50=37.8211 μM SANGER
EW-22 Growth Inhibition Assay IC50=42.2885 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=42.7853 μM SANGER
ES3 Growth Inhibition Assay IC50=43.1339 μM SANGER
EW-11 Growth Inhibition Assay IC50=44.8218 μM SANGER
RH-1 Growth Inhibition Assay IC50=47.5812 μM SANGER
HepG2 Function assay Inhibition of human HepG2 cells, IC50 = 0.0009 μM. 18247554
HEK293 Function assay Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells, IC50 = 0.12 μM. 19441846
HEK293 Function assay Inhibition of HDAC1 in HEK293 cells, IC50 = 0.12 μM. 18308563
SNU16 Function assay Inhibition of HDAC from human SNU16 cells, IC50 = 0.233 μM. 18247554
HEK293 Function assay Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells, IC50 = 0.25 μM. 19441846
U937 Function assay Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay, IC50 = 0.3 μM. 18381238
HEK293 Function assay Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells, IC50 = 0.4 μM. 19441846
HEK293 Function assay Inhibition of HDAC3 in HEK293 cells, IC50 = 0.4 μM. 18308563
HCT116 Function assay Inhibition of human HCT116 cells, IC50 = 0.5 μM. 18247554
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells, IC50 = 0.67 μM. 21742496
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.67 μM. 21650221
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay, IC50 = 0.7 μM. 18370373
ML1 Antitumor assay Antitumor activity against mouse ML1 cells, IC50 = 0.75 μM. 19534534
SKBR3 Antiproliferative assay Antiproliferative activity against human SKBR3 cells, IC50 = 0.87 μM. 18247554
S2 Function assay Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.94 μM. 19317450
A549 Antiproliferative assay Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay, IC50 = 1.2 μM. 18370373
G401 Antiproliferative assay Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay, IC50 = 1.3 μM. 18370373
HeLa Antiproliferative assay Antiproliferative activity against HeLa cells by alamar blue assay, IC50 = 1.58489 μM. 17606370
HeLa Antiproliferative assay Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay, IC50 = 1.8 μM. 18370373
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by MTT assay, IC50 = 2 μM. 19131248
K562 Function assay Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells., IC50 = 2 μM. 12419380
K562 Function assay Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells, IC50 = 2 μM. 14592473
SNU-16 Function assay Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells, IC50 = 2.19459 μM. 14667227
A2780 Antiproliferative assay Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay, IC50 = 3 μM. 18370373
SW620 Function assay Inhibition of human SW620 cells, IC50 = 3.2 μM. 18247554
A549 Antiproliferative assay Antiproliferative activity against human A549 cells, IC50 = 3.58 μM. 18247554
MKN45 Antiproliferative assay Antiproliferative activity against human MKN45 cells, IC50 = 4.16 μM. 18247554
MCF7 Function assay Inhibition of human MCF7 cells, IC50 = 4.3 μM. 18247554
K562 Function assay Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells., IC50 = 4.8 μM. 10425110
HeLa Function assay Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation, IC50 = 4.8 μM. 19534534
HeLa Function assay Inhibition of HDAC in HeLa cells, IC50 = 12.5892 μM. 17606370
U937 Function assay Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay. 18381238
U937 Function assay Induction of histone H4 hyperacetylation in human U937 cells. 18381238
U937 Function assay Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay. 18381238
U937 Function assay Induction of granulocytic differentiation in human U937 cells. 18381238
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells. 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells. 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells. 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells. 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells. 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells. 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells. 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells. 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells. 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells. 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells. 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells. 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells. 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells. 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells. 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells. 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells. 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells). 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells. 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells. 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells. 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells. 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells. 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells. 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells. 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells. 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells. 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells. 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells. 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells. 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells. 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells. 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells. 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells. 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells. 29435139
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生物活性

產(chǎn)品描述 Entinostat (MS-275, SNDX-275)強(qiáng)烈抑制HDAC1和HDAC3，無細(xì)胞試驗(yàn)中IC50分別為0.51 μM和1.7 μM，抑制作用強(qiáng)于HDACs 4， 6， 8，和10。Entinostat可誘導(dǎo)自噬和凋亡。Phase 3。
靶點(diǎn)
HDAC1 [2]
(Cell-free assay)		 HDAC3 [2]
(Cell-free assay)
0.51 μM 1.7 μM
體外研究(In Vitro)
體外研究活性 MS-275通過作用于2′-氨基而抑制HDACs。MS-275作用于 K562細(xì)胞，誘導(dǎo) p21WAF1/CIP1和凝溶膠蛋白的累積。MS-275作用于A2780細(xì)胞，可以降低S期細(xì)胞，提高G1期細(xì)胞。 MS-275通過抑制HAD而抑制人類腫瘤細(xì)胞系，包括 A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St和 HCT-15細(xì)胞增殖， IC50 為41.5 nM到4.71 μM。[1]MS-275抑制HDACs，作用于HDAC1和 HDAC3時IC50 分別為0.51 μM和1.7 μM。而對其他的HDACs沒有抑制效果，如HDAC4, 6, 8和10。[2]MS-275有效抑制人類白血病和淋巴癌細(xì)胞，包括U937, HL-60, K562, 和Jurkat。MS-275可以誘導(dǎo)U937細(xì)胞p21CIP1/WAF1 調(diào)節(jié)的生長和變異Marker (CD11b)的表達(dá)。MS-275降低cyclin D1和抗凋亡蛋白Mcl-1與XIAP的表達(dá)。[3]
激酶實(shí)驗(yàn) 標(biāo)準(zhǔn)HDAC實(shí)驗(yàn)
用HDAC buffer按1:6稀釋鼠肝內(nèi)的酶。重組人類HDACs按1:4稀釋在HDAC buffer中。用于標(biāo)準(zhǔn)HDAC實(shí)驗(yàn)，60 μl HDAC buffer和10 μl 稀釋的酶溶液在30oC混合。在HDAC buffer中加入30 μl基底液開始HDAC反應(yīng)，隨后在30oC下溫育30分鐘。加入100 μl胰蛋白酶溶液終止反應(yīng)，胰蛋白酶溶液由溶于50 mM Tris-HCl（pH 為8.0）的10 mg/ml 胰蛋白酶, 100 mM NaCl,及 2 μM TSA組成。30oC下溫育20分鐘， 通過測定460納米(λex = 390 nm)處的熒光監(jiān)測AMC的釋放。使用釋放的AMC校準(zhǔn)熒光強(qiáng)度 。用于標(biāo)準(zhǔn)時間過程實(shí)驗(yàn)，在初始100 μl HDAC 反應(yīng)中加入20 pmol 基底物。2-50 pmol 基底物的酶法分析產(chǎn)物獲得熒光AMC，通過測量這種熒光AMC來測定 Km值和 Vmax值。使用Hanes 圖分析實(shí)驗(yàn)數(shù)據(jù)。記錄的AMC信號是針對沒有酶而有buffer和基底物的空白區(qū)。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St和HCT-15細(xì)胞
濃度 10 μM 左右
孵育時間 3天
方法 5×103個腫瘤細(xì)胞接種到96孔板上，加入梯度濃度MS-275培養(yǎng)三天。細(xì)胞用0.1 mg/mL中性紅在CO2反應(yīng)器中染色1小時，測定中性紅與50 μL乙醇和150 μL 0.1 M Na2HPO4溶解后的OD540,測定IC50值。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3 Cleaved PARP Caspase 8 DR4 / DR5 TopoIIα / TopoIIβ 24203492
Immunofluorescence phalloidin / snail DR4 / DR5 H3K4Me3 / H3K9Me3 29855565
Growth inhibition assay Cell proliferation Cell viability 24203492
ELISA GCP-2 / MCP-2 / MIF 24241152
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 MS-275按49 mg/kg劑量作用于除了HCT-15的人類移植瘤都顯示出強(qiáng)抗癌活性。[1]MS-275促進(jìn)惡性實(shí)體瘤和惡性血液病的治療可能性，及生理和畸變基因表達(dá)的調(diào)節(jié)。[4]MS-275和IL-2聯(lián)用，作用于腎細(xì)胞癌顯示出強(qiáng)抗癌活性，因?yàn)榻档驼{(diào)節(jié)性T細(xì)胞和增強(qiáng)脾細(xì)胞的表達(dá)。[5]
動物實(shí)驗(yàn) Animal Models 側(cè)腹皮下注射A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1和Calu-3細(xì)胞的裸鼠
Dosages 12.3, 24.5和49 mg/kg
Administration 每天口服處理一次，每周進(jìn)行5天，持續(xù)4周。
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04708470 Recruiting
Oropharyngeal Cancer|Neck Cancer|Human Papillomavirus|HPV|Anal Cancer|Cervical Cancer|Penile Cancer|Vulvar Cancer|Vaginal Cancer|Colon Cancer
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 October 5 2021 Phase 1|Phase 2
NCT03829930 Terminated
Prostate Adenocarcinoma
George Washington University
 May 1 2019 Phase 1
NCT03765229 Completed
Melanoma
UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals
 March 22 2019 Phase 2
NCT03473639 Completed
Metastatic Breast Cancer|Breast Cancer
University of Virginia|Syndax Pharmaceuticals
 January 29 2019 Phase 1

化學(xué)信息&溶解度

分子量 376.41 分子式

C21H20N4O3
CAS號 209783-80-2 SDF Download Entinostat (MS-275) SDF
Smiles C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 75 mg/mL ( (199.25 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
I would like to use Entinostat（Catalog No.S1053） for animal study. What is your recommendation for the solvent? What is the role of PEG 300 in this case? Can I use DMSO only and dilute it with PBS or HBSS?

回答：
2%DMSO/30%PEG/68%Water is recommended. PEG is an important polymer that helps with the solubility of hydrophobic drugs. If you use DMSO only and dilute it with PBS or HBSS, Entinostat will likely to precipitate out since it has very low solubility in water.

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