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Romidepsin

別名: FK228, Depsipeptide, FR 901228, NSC 630176, 中文名稱：羅米地辛

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)是一種有效的HDAC1和HDAC2抑制劑，無細(xì)胞試驗(yàn)中IC50分別為36 nM和47 nM。Romidepsin (FK228/depsipeptide) 在神經(jīng)母細(xì)胞瘤腫瘤細(xì)胞中可控制生長并誘導(dǎo)凋亡。

Romidepsin Chemical Structure

Romidepsin Chemical Structure

CAS: 128517-07-7

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 4013.1 現(xiàn)貨
1mg 1203.93 現(xiàn)貨
5mg 3030.3 現(xiàn)貨
10mg 4905.81 現(xiàn)貨
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Romidepsin 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
A549 Growth Inhibition Assay 5 nM 24/48/72 h inhibits cell growth time-dependently 22106282
LNCaP Growth Inhibition Assay 5 nM 24/48/72 h inhibits cell growth time-dependently 22106282
HFS Growth Inhibition Assay 5 nM 24/48/72 h inhibits cell growth time-dependently 22106282
CO115 Growth Inhibition Assay 5 nM-50 μM 24 h inhibits cell growth in a concentration-dependent manner 22924958
RKO Growth Inhibition Assay 5 nM-50 μM 24 h inhibits cell growth in a concentration-dependent manner 22924958
HCT116 Growth Inhibition Assay 5 nM-50 μM 24 h inhibits cell growth in a concentration-dependent manner 22924958
NCI/ADR-RES Growth Inhibition Assay 1–20nM 72 h reduces cell viability alone and combined with cisplatin 23010348
OVCAR-8? Growth Inhibition Assay 1–20nM 72 h reduces cell viability alone and combined with cisplatin 23010348
Brca1 Null Growth Inhibition Assay 1–20nM 72 h reduces cell viability alone and combined with cisplatin 23010348
Brca1 WT Growth Inhibition Assay 1–20nM 72 h reduces cell viability alone and combined with cisplatin 23010348
SKOV-3 Growth Inhibition Assay 1–20nM 72 h reduces cell viability alone and combined with cisplatin 23010348
DpP75? Apoptosis Assay 1/10/100 nM 48 h induces blunt apoptosis 23532732
DpVp50 Apoptosis Assay 1/10/100 nM 48 h induces blunt apoptosis 23532732
DpVp35 Apoptosis Assay 1/10/100 nM 48 h induces blunt apoptosis 23532732
HuT78 Apoptosis Assay 1/10/100 nM 48 h induces apoptosis at 1 nM 23532732
A549 Growth Inhibition Assay 10–100?nM 24/36/48 h inhibits cell growth in both concentration- and time-dependent manner 24485799
MS-275 Growth Inhibition Assay 0.625-10nM 48 h induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib 24771510
HA Growth Inhibition Assay 0.625-10nM 48 h induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib 24771510
ACH-2 Function Assay 1-9 nM 24 h induces HIV-1 Env expression 25149467
HCT116 Growth Inhibition Assay 5-5000 nM 24 h induces cell death in a concentration-dependent manner 25492515
U2932/EBV Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner? 25790907
LY7/EBV Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner? 25790907
Farage Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner? 25790907
OCI-LY7 Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner? 25790907
U2932? Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner? 25790907
SU-DHL4 Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner? 25790907
THJ-16T Growth Inhibition Assay 1 nM 24 h inhibits cell growth 20810568
HCT116 Function Assay 20 nM 8 h modulates transcript levels for hundreds of genes in either direction 20739454
B104? Function Assay 2 nM 24/48/72 h increases the surface expression of CD20? 20686505
HL-60? Cytotoxicity Assay 1-500 nM 24 h induces cytotoxicity in a concentration-dependent manner? 20624163
HP100 Cytotoxicity Assay 1-500 nM 24 h induces cytotoxicity in a concentration-dependent manner? 20624163
HL-60? Function Assay 10 nM 4/6/16 h induces the generation of hydrogen peroxide from 4h 20624163
HP100 Function Assay 10 nM 4/6/16 h induces the generation of hydrogen peroxide from 4h 20624163
HL-60? Function Assay 10-500 nM 4 h decreases the histone deacetylase (HDAC) activity? 20624163
HP100 Function Assay 10-500 nM 4 h decreases the histone deacetylase (HDAC) activity? 20624163
SKOV-3 Growth Inhibition Assay 4/8/16 nM 48 h inhibits cell growth in a concentration-dependent manner 20404564
OVCAR-3 Growth Inhibition Assay 4/8/16 nM 48 h inhibits cell growth in a concentration-dependent manner 20404564
HBL-2 Growth Inhibition Assay 2-10 nM 24 h IC50=4.3 nM 20068080
Jeko-1 Growth Inhibition Assay 2-50 nM 24 h IC50=11 nM 20068080
Granta-519 Growth Inhibition Assay 5-40 nM 24 h IC50=58.5 nM 20068080
L1236 Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.07 μM 19233470
L428 Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.43 μM 19233470
KM-H2 Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.58 μM 19233470
L540Cy Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.16 μM 19233470
G401 Function Assay 10 nM 24/48/72 h increases CDKN1C expression 19221586
STM91-01 Function Assay 10 nM 24/48/72 h increases CDKN1C expression 19221586
SJSC? Function Assay 10 nM 24/48/72 h increases CDKN1C expression 19221586
BT16? Function Assay 10 nM 24/48/72 h increases CDKN1C expression 19221586
NCI-H23 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
NCI-H522 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
OVCAR5 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
SW620 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
MDA-MB-435 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
COLO205 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
LOXIMVI Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
UACC62 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
MDA-MB-231 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
SF295 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
U251 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
OVRAC3 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
11z Kinase Assay 3-100 nM reduces HDAC enzymatic activity (IC50?= 6.5 ± 0.6 nmol/L) 20605144
ST486 Apoptosis Assay 6 h induces extensive apoptosis 23966164
Ramos Apoptosis Assay 6 h induces extensive apoptosis 23966164
DG75 Apoptosis Assay 6 h induces no apoptosis 23966164
CA46 Apoptosis Assay 6 h induces blunt apoptosis 23966164
U266 Growth Inhibition Assay 24/48 h EC50s=10?nM; 48?h 24030150
RPMI-8226 Growth Inhibition Assay 24/48 h EC50s=1.8?nM; 48?h 24030150
OPM-2 Growth Inhibition Assay 24/48 h EC50s=1?nM; 48?h 24030150
JJN3 Growth Inhibition Assay 24/48 h EC50<1?nM; 48?h 24030150
CD4 T Growth Inhibition Assay 48 h CC50=107±126 nM 24722454
CD4 T Growth Inhibition Assay 48 h EC50=4.5±1.0 nM 24722454
A498 Cytotoxicity assay 6 days Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM. 21967146
COLO205 Cytotoxicity assay 6 days Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM. 21967146
U251 Cytotoxicity assay 6 days Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM. 21967146
RXF393 Cytotoxicity assay 6 days Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM. 21967146
MDA-MB-468 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM. 21967146
COLO205 Cytotoxicity assay 6 days Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM. 21967146
UACC257 Cytotoxicity assay 6 days Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM. 21967146
U251 Cytotoxicity assay 6 days Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM. 21967146
A498 Cytotoxicity assay 6 days Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM. 21967146
NCI-H322M Cytotoxicity assay 6 days Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM. 21967146
SF295 Cytotoxicity assay 6 days Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM. 21967146
RXF393 Cytotoxicity assay 6 days Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM. 21967146
NCI60 Cytotoxicity assay 6 days Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM. 21967146
SN12C Cytotoxicity assay 6 days Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM. 21967146
MDA-MB-231 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM. 21967146
ACHN Cytotoxicity assay 6 days Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM. 21967146
SN12C Cytotoxicity assay 6 days Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM. 21967146
UO31 Cytotoxicity assay 6 days Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM. 21967146
Caki1 Cytotoxicity assay 6 days Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM. 21967146
NCI60 Cytotoxicity assay 6 days Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM. 21967146
MDA-MB-231 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM. 21967146
MDA-MB-468 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM. 21967146
ACHN Cytotoxicity assay 6 days Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM. 21967146
UACC257 Cytotoxicity assay 6 days Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM. 21967146
NCI-H322M Cytotoxicity assay 6 days Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM. 21967146
SF295 Cytotoxicity assay 6 days Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM. 21967146
Caki1 Cytotoxicity assay 6 days Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM. 21967146
CD4+ T Function assay 7 days Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM. 24495105
293T Function assay 30 mins Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM. 24589486
293T Function assay 30 mins Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM. 24589486
mink Mv1Lu Function assay 24 hrs Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM. 24997578
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM. 25147612
MOLT4 Antiproliferative assay 72 hrs Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM. 26331334
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM. 26331334
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM. 26331334
HLF Antiproliferative assay 72 hrs Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM. 26331334
WI38 Antiproliferative assay 72 hrs Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM. 26331334
U937 Function assay 24 hrs Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis 26331334
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM. 26481659
IGROV1/Pt1 Antiproliferative assay 72 hrs Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM. 26481659
IGROV1 Antiproliferative assay 72 hrs Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM. 26481659
CD4+ T Growth Inhibition Assay EC50=3 nM 24495105
HuT-78 Growth Inhibition Assay IC50=1.73±0.44 nM 24954856
H526 Growth Inhibition Assay IC50=0.15±0.03 nM 24954856
H146 Growth Inhibition Assay IC50=0.22±0.07 nM 24954856
EKVX Growth Inhibition Assay IC50=1.33±0.34 nM 24954856
H460 Growth Inhibition Assay IC50=2.58±0.80 nM 24954856
A549 Growth Inhibition Assay IC50=1.26±0.24 nM 24954856
SF-295 Growth Inhibition Assay IC50=0.88±0.15 nM 24954856
MDA-MB-435 Growth Inhibition Assay IC50=0.90±0.06 nM 24954856
UACC-62 Growth Inhibition Assay IC50=0.56±0.16 nM 24954856
LOX-IMVI Growth Inhibition Assay IC50=0.87±0.03 nM 24954856
SW620 Growth Inhibition Assay IC50=0.93±0.29 nM 24954856
S1 Growth Inhibition Assay IC50=7.67±0.29 nM 24954856
HCT116-p21-/- Growth Inhibition Assay IC50=1.26±0.37 nM 24954856
HCT116 Growth Inhibition Assay IC50=1.00±0.00 nM 24954856
PC3 Growth Inhibition Assay IC50=1.65±0.35 nM 24954856
MDA-MB-231 Growth Inhibition Assay IC50=0.68±0.14 nM 24954856
SK-BR-3 Growth Inhibition Assay IC50=1.00±0.35 nM 24954856
MCF-7 Growth Inhibition Assay IC50=1.10±0.20 nM 24954856
MCF-10A Growth Inhibition Assay IC50=0.17±0.01 nM 24954856
697? Growth Inhibition Assay IC50?=?2.5?nM 21538216
697-R Growth Inhibition Assay IC50?=?8.6?nM? 21538216
HUT78 Growth Inhibition Assay IC50=1 nM 21198545
NCI-H1299 Growth Inhibition Assay IC50=4.6±0.2 ng/ml 19179890
NCI-2882 Growth Inhibition Assay IC50=1.6±0.04 ng/ml 19179890
HCC95 Growth Inhibition Assay IC50=2.5±0.05 ng/ml 19179890
NCI-H23 Growth Inhibition Assay IC50=2.9±0.2 ng/ml 19179890
NCI-H157 Growth Inhibition Assay IC50=1.6±0.02 ng/ml 19179890
NCI-H460 Growth Inhibition Assay IC50=2.1±0.07 ng/ml 19179890
NCI-H1975 Growth Inhibition Assay IC50=1.3±0.04 ng/ml 19179890
NCI-H820 Growth Inhibition Assay IC50=2.4±0.1 ng/ml 19179890
NCI-H1650 Growth Inhibition Assay IC50=4.9±0.3 ng/ml 19179890
DTC1 Growth Inhibition Assay IC50=0.51 nM 18566246
KAO Growth Inhibition Assay IC50=0.91 nM 18566246
SU-CCS-1 Growth Inhibition Assay IC50=0.89 nM 18566246
SYO-1 Growth Inhibition Assay IC50=0.67 nM 18566246
FUJI Growth Inhibition Assay IC50=1.31 nM 18566246
SKNMC Growth Inhibition Assay IC50=1.17 nM 18566246
402-91 Growth Inhibition Assay IC50=1.26 nM 18566246
1765-92 Growth Inhibition Assay IC50=1.77 nM 18566246
JN-DSRCT-1 Growth Inhibition Assay IC50=1.25 nM 18566246
NMS-2PC Growth Inhibition Assay IC50=0.81 nM 18566246
HL60 Growth Inhibition Assay IC50=1.86 nM 18566246
A549 Growth Inhibition Assay IC50=3.24 nM 18566246
SW480 Growth Inhibition Assay IC50=2.69 nM 18566246
MCF7 Growth Inhibition Assay IC50=3.55 nM 18566246
PC-3 Growth Inhibition Assay IC50=2.51 nM 18566246
MMRU Growth Inhibition Assay IC50=2.57 nM 18566246
Hs68 Growth Inhibition Assay IC50=>10 nM 18566246
hMSC-001F Growth Inhibition Assay IC50=>10 nM 18566246
mammalian cells Function assay Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM. 14584932
mammalian cells Function assay Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM. 14584932
MCF7 Growth inhibition assay Growth inhibition of MCF7 cells, IC50 = 0.00075 μM. 17958342
LLC Function assay Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM. 22305612
NCI-H522 Growth inhibition assay Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM. 23313638
LOXIMVI Growth inhibition assay Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM. 23313638
A549 Growth inhibition assay Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM. 23313638
OVCAR5 Growth inhibition assay Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM. 23313638
MKN74 Growth inhibition assay Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. 23313638
NCI-H460 Growth inhibition assay Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. 23313638
HCT116 Growth inhibition assay Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. 23313638
HCC2998 Growth inhibition assay Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. 23313638
MKN1 Growth inhibition assay Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM. 23313638
SKOV3 Growth inhibition assay Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. 23313638
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. 23313638
KM12 Growth inhibition assay Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM. 23313638
DMS114 Growth inhibition assay Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. 23313638
SF539 Growth inhibition assay Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. 23313638
U251 Growth inhibition assay Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM. 23313638
SF295 Growth inhibition assay Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM. 23313638
MCF7 Growth inhibition assay Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM. 23313638
NCI-H23 Growth inhibition assay Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. 23313638
OVCAR3 Growth inhibition assay Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. 23313638
MKN7 Growth inhibition assay Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. 23313638
SF268 Growth inhibition assay Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. 23313638
MDA-MB-231 Growth inhibition assay Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. 23313638
OVCAR8 Growth inhibition assay Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. 23313638
DMS273 Growth inhibition assay Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM. 23313638
DU145 Growth inhibition assay Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM. 23313638
RXF631L Growth inhibition assay Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM. 23313638
HBC4 Growth inhibition assay Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM. 23313638
SNB75 Growth inhibition assay Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM. 23313638
BSY1 Growth inhibition assay Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM. 23313638
NCI-H226 Growth inhibition assay Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM. 23313638
SNB78 Growth inhibition assay Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM. 23313638
HBC5 Growth inhibition assay Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM. 23313638
MKN45 Growth inhibition assay Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM. 23313638
MKN28 Growth inhibition assay Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM. 23313638
PC3 Growth inhibition assay Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM. 23313638
ACHN Growth inhibition assay Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. 23313638
OVCAR4 Growth inhibition assay Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. 23313638
St-4 Growth inhibition assay Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM. 23313638
HCT15 Growth inhibition assay Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM. 23313638
NCI-H522 Cytotoxicity assay Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM. 24589486
LOXIMVI Cytotoxicity assay Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM. 24589486
A549 Cytotoxicity assay Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM. 24589486
OVCAR5 Cytotoxicity assay Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM. 24589486
NCI-H460 Cytotoxicity assay Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM. 24589486
MKN74 Cytotoxicity assay Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM. 24589486
HCC2998 Cytotoxicity assay Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM. 24589486
HCT116 Cytotoxicity assay Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM. 24589486
MKN1 Cytotoxicity assay Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM. 24589486
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM. 24589486
SKOV3 Cytotoxicity assay Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM. 24589486
KM12 Cytotoxicity assay Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM. 24589486
SF539 Cytotoxicity assay Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM. 24589486
DMS114 Cytotoxicity assay Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM. 24589486
U251 Cytotoxicity assay Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM. 24589486
SF295 Cytotoxicity assay Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM. 24589486
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM. 24589486
OVCAR3 Cytotoxicity assay Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM. 24589486
NCI-H23 Cytotoxicity assay Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM. 24589486
SF268 Cytotoxicity assay Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM. 24589486
MKN7 Cytotoxicity assay Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM. 24589486
OVCAR8 Cytotoxicity assay Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM. 24589486
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM. 24589486
DMS273 Cytotoxicity assay Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM. 24589486
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM. 24589486
RXF631L Cytotoxicity assay Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM. 24589486
HBC4 Cytotoxicity assay Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM. 24589486
SNB75 Cytotoxicity assay Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM. 24589486
BSY1 Cytotoxicity assay Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM. 24589486
NCI-H226 Cytotoxicity assay Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM. 24589486
SNB78 Cytotoxicity assay Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM. 24589486
HBC5 Cytotoxicity assay Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM. 24589486
MKN45 Cytotoxicity assay Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM. 24589486
MKN28 Cytotoxicity assay Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM. 24589486
PC3 Cytotoxicity assay Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM. 24589486
ACHN Cytotoxicity assay Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM. 24589486
OVCAR4 Cytotoxicity assay Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM. 24589486
St-4 Cytotoxicity assay Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM. 24589486
HCT15 Cytotoxicity assay Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM. 24589486
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生物活性

產(chǎn)品描述 Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)是一種有效的HDAC1和HDAC2抑制劑，無細(xì)胞試驗(yàn)中IC50分別為36 nM和47 nM。Romidepsin (FK228/depsipeptide) 在神經(jīng)母細(xì)胞瘤腫瘤細(xì)胞中可控制生長并誘導(dǎo)凋亡。
特性 Romidepsin對I型HDAC的抑制作用明顯強(qiáng)于對II型HDAC的抑制。
靶點(diǎn)
HDAC1 [1]
(Cell-free assay)		 HDAC2 [1]
(Cell-free assay)
36 nM 47 nM
體外研究(In Vitro)
體外研究活性 Romidepsin抑制NSCLC細(xì)胞系生長，IC50范圍從1.3 ng/mL到4.9 ng/mL。 Romidepsin可以降低Erlotinib對NSCLC細(xì)胞系的IC50值， 增加NSCLC細(xì)胞系對Erlotinib的敏感性[1]。Romidepsin處理72小時可以抑制6/6 人 NB 腫瘤細(xì)胞系的生長，而 NIH3T3細(xì)胞系并不受影響。 Romidepsin對于單拷貝或N-myc 多拷貝的NB細(xì)胞系以及含有正常或突變的p53 和含有Alk突變體的細(xì)胞系都有選擇性的細(xì)胞毒性，這種毒性具有劑量依賴的特性。[2]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 NCI-H1975, NCI-H157, NCI-2882, NCI-H460 和 HCC95 細(xì)胞系
濃度 1 ng/mL
孵育時間 72 小時
方法 使用MTS法分析藥物敏感性。在96孔平板中每孔接種2×103個細(xì)胞(包括NCI-H1975, NCI-H157, NCI-2882, NCI-H460和HCC95) 。24小時后, 在存在或者缺少1 ng/mL Romidepsin的條件下將細(xì)胞與不同濃度 (0.01 μM - 250 μM) 的Erlotinib 37°C 孵育72 小時。 MTS 溶液加到每個孔中37°C孵育1小時。利用分光光度計測量490 nm 處的光密度值。每種藥物濃度的實(shí)驗(yàn)都設(shè)置8個復(fù)孔并重復(fù)兩次?；诩?xì)胞生存曲線的吸光度值計算藥物的半抑制濃度 (IC50) 。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT 19682393
Growth inhibition assay Cell viability 27444036
Immunofluorescence SS18/TLE1 Cleaved caspase-3 27120803
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 與PBS處理的對照組相比，單獨(dú)使用Erlotinib 和 Romidepsin分別可以對NCI-H1299細(xì)胞系的異種移植生長抑制到72% 和 43% ，但是并不具有明顯的統(tǒng)計學(xué)意義。只有當(dāng)兩種藥物聯(lián)用的時候才會對其生長造成明顯的抑制作用，此時生長被抑制到28% [1]。在免疫功能低下的小鼠中，Romidepsin 會抑制皮下NB 異種移植的生長，這種抑制作用具有劑量依賴的特性 。此外, 在NB病人的腫瘤組織中Romidepsin 會誘導(dǎo)某些基因的表達(dá)，如 p21 和p75 以及NTRK (TrkA) [2]。
動物實(shí)驗(yàn) Animal Models 攜帶NCI-H1299 細(xì)胞的 BALB/c無胸腺裸小鼠
Dosages 1.2 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03770000 Completed
T Cell Lymphoma
Rhizen Pharmaceuticals SA
 March 12 2019 Phase 1|Phase 2
NCT02616965 Active not recruiting
Cutaneous T-cell Lymphoma (CTCL)
Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation
 February 22 2017 Phase 1
NCT02616874 Completed
HIV
IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint
 February 2016 Phase 1

化學(xué)信息&溶解度

分子量 540.7 分子式

C24H36N4O6S2
CAS號 128517-07-7 SDF --
Smiles CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (184.94 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)配方計算器

實(shí)驗(yàn)計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（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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