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Silmitasertib (CX-4945)

Silmitasertib (CX-4945)是有效的，選擇性CK2(casein kinase 2)抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為1 nM,對(duì) Flt3, Pim1 和 CDK1作用效果稍弱(細(xì)胞試驗(yàn)中沒有活性)。Silmitasertib可誘導(dǎo)自噬并促進(jìn)細(xì)胞凋亡。Phase 1/2。

Silmitasertib (CX-4945) Chemical Structure

Silmitasertib (CX-4945) Chemical Structure

CAS: 1009820-21-6

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 2104.83 現(xiàn)貨
2mg 958.23 現(xiàn)貨
5mg 1711.71 現(xiàn)貨
50mg 7289.1 現(xiàn)貨
1g 30221.58 現(xiàn)貨
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常與Silmitasertib (CX-4945)一起在實(shí)驗(yàn)中被使用的化合物

Venetoclax (ABT-199)

Silmitasertib和Venetoclax組合可增加套細(xì)胞淋巴瘤(MCL)細(xì)胞凋亡。

Manni S, et al. Hemasphere 6 (2022): 1164-1165.

Trabectedin

Silmitasertib和Trabectedin可降低黑素瘤細(xì)胞系MM66/MP46/MP38/MM28中Bcl-2的表達(dá)，并增加Bim和Bmf的表達(dá)。

Glinkina K, et al. Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14.

Imatinib

Silmitasertib和Imatinib聯(lián)合抑制CK2和KIT，導(dǎo)致GIST882，GIST430/654和GIST48細(xì)胞中KIT/PI3K/AKT/mTOR失活。

Huang M, et al. Br J Cancer. 2020 Feb;122(3):372-381.

Decitabine

Silmitasertib(CX-4945)和Decitabine聯(lián)合使用可減少PTEN和AKT磷酸化，并抑制PI3K/AKT介導(dǎo)的體外和體內(nèi)增殖。

Richter A, et al. BMC Cancer. 2019 Mar 6;19(1):202.

Silmitasertib (CX-4945)相關(guān)產(chǎn)品

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(shí)間 活性描述 文獻(xiàn)信息
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
A549 Function assay 10 uM 4 to 24 hrs Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method 24012124
A549 Function assay 10 uM 24 hrs Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method 24012124
A549 Function assay 10 uM Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method 24012124
A549 Function assay 10 uM 15 to 30 mins Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method 24012124
A549 Function assay 30 uM 48 hrs Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography 24012124
Vero E6 Antiviral assay 48 h IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 3.89045 μM. 32353859
Sf21 Function assay 90 mins Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay, IC50 = 0.003 μM. 29559278
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50 = 9.9 μM. 26850376
Sf9 Function assay Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP, IC50 = 1.8 μM. 24681986
K562 Antiproliferative assay 1 to 3 days Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50 = 7 μM. 23711832
U937 Antiproliferative assay 1 to 3 days Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50 = 4.2 μM. 23711832
MV4-11 Antiproliferative assay 1 to 3 days Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50 = 3 μM. 23711832
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50 = 8.2 μM. 22339433
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 6.5 μM. 22339433
Hs 578T Antiproliferative assay 4 days Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50 = 13.1 μM. 21174434
MCF7 Antiproliferative assay 4 days Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50 = 8.9 μM. 21174434
MDA-MB-231 Antiproliferative assay 4 days Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50 = 6.4 μM. 21174434
LNCAP Antiproliferative assay 4 days Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50 = 4.7 μM. 21174434
BxPC3 Antiproliferative assay 4 days Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50 = 4.4 μM. 21174434
A549 Antiproliferative assay 4 days Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50 = 3 μM. 21174434
Jurkat Antiproliferative assay 4 days Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50 = 2.5 μM. 21174434
HCT116 Antiproliferative assay 4 days Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50 = 2.2 μM. 21174434
MIAPaCa2 Antiproliferative assay 4 days Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50 = 1.1 μM. 21174434
Jurkat Function assay Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50 = 0.1 μM. 21174434
HDMEC Function Assay 1 μM 24 h affects subcellular localization of NFATc1 and phospho-p65 26381437
HDMEC Function Assay 0.25/0.5/1 μM 24 h reduces expression of VCAM-1 but not ICAM-1 26381437
A549? Function Assay 3/10?μM 48 h suppresses the micropillar-induced expression of p-FAK 26318800
HDMEC Function Assay 50 μM 1/5 h decreases the nuclear signal of phosphorylated p65 in TNF-α-stimulated HDMEC? 26189586
HDMEC Kinase Assay 1-50 μM 5 h decreases CK2 kinase activity without affecting cell viability 26189586
HEK293 Function Assay 3 μM 5 h CK2 phosphorylates eIF3j at Ser127 25887626
LAMA84 Kinase Assay 0.5?μM 15 min reduces CK2 kinase activity 25887626
Hela Kinase Assay 0.5?μM 15 min reduces CK2 kinase activity 25887626
HEK293 Kinase Assay 0.5?μM 15 min reduces CK2 kinase activity 25887626
UM-SCC46 Function Assay 0.5/4/10 μM 72 h down-regulates the expression of NF-?B, Bcl-XL, p53, p21, AP-1 and up-regulates the expression IL-8 concentration dependently 25798061
UM-SCC1 Function Assay 0.5/4/10 μM 72 h down-regulates the expression of NF-?B, Bcl-XL and up-regulates the expression of p53, p21, AP-1 and IL-8 concentration dependently 25798061
UM-SCC46 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=3.4 μM 25798061
Raji Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 19? Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 18 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 1 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 10 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 3 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
NU-DUL Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
H358 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
Calu-1? Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
PC9/ER Function Assay 5 μM 48 h induces autophagy 25486409
PC9/GR Function Assay 5 μM 48 h induces autophagy 25486409
H2052 Growth Inhibition Assay 0.01-30 μM 72 h IC50=2.0 μM 25422081
UM-SCC-46 Clonogenic Assay 0.5-5 μM 14 d ?inhibits clonogenic survival and sphere formation 25379016
H2170? Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
A431? Function Assay 10 μM 4-24 h enhances apoptosis with 22387988
H2170? Function Assay 10 μM 4-24 h enhances apoptosis with 22387988
LNCap Growth Inhibition Assay 0-30 μM 4 d IC50=4.59?μM 22832316
A549 Growth Inhibition Assay 0-30 μM 72 h IC50=4.15 μM, inhibits cell growth concentration dependently 23651443
H1299 Growth Inhibition Assay 0-30 μM 72 h IC50=1.80 μM, inhibits cell growth concentration dependently 23651443
A549 Function Assay 1/10 μM 48 h leads to a dose-dependent decrease in Notch reporter activity 23651443
S-LAMA84 Function Assay 3?μM 24 h reduces CK2 activity 24012109
A549 Function Assay 10 μM 12/24/48 h inhibits TGF-β1-induced migration and invasion 24023938
A549 Function Assay 3 μM 48 h inhibits TGF-β1-induced activation of Smad and expression of Snail and Twist 24023938
U-266 Growth Inhibition Assay 0-40 μM 48 h IC50=19.8 μM? 24086494
Jeko-1 Growth Inhibition Assay 0-40 μM 48 h IC50=2.4 μM? 24086494
INA-6 Growth Inhibition Assay 0-40 μM 48 h IC50=2.42 μM 24086494
Rec-1 Growth Inhibition Assay 0-40 μM 48 h IC50=1.46 μM? 24086494
CEM-R Growth Inhibition Assay 1-10 μM 48 h IC50=4 μM 24253024
Jurkat Growth Inhibition Assay 1-10 μM 48 h IC50=4.9 μM 24253024
CEM-S Growth Inhibition Assay 1-10 μM 48 h IC50=4.6 μM 24253024
MOLT-4 Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
PF-382 Growth Inhibition Assay 1-10 μM 48 h IC50=4.5 μM 24253024
ALL-SIL Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
DND-41 Growth Inhibition Assay 1-10 μM 48 h IC50=9 μM 24253024
HPB-ALL Growth Inhibition Assay 1-10 μM 48 h IC50=6.1 μM 24253024
ALL-SIL Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
DND-41 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
MOLT-4 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
C2C12 Function Assay 3 μM 12/24/48 h inhibits the expression of osteoclast differentiation markers and Akt phosphorylation 24293011
Nalm6? Function Assay 10/20 μM 24 h results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression 24561792
SUP-B15 Function Assay 10/20 μM 24 h results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression 24561792
SUP-B15 Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
ARPE-19 Kinase Assay 5/10/20 μM 24/48 h inhibits CK2 kinase activity at a concentration of 5?μM 24686080
ARPE-19 Growth Inhibition Assay 10 μM 24-96 h inhibits cell growth time dependently 24686080
HCT116? Growth Inhibition Assay 10 μM 24-96 h inhibits cell growth time dependently 24686080
ARPE-19 Function Assay 10 μM 4 h causes ER-stress response over the p-eIF2α branch, but does not induce CHOP? 24686080
HCT116? Function Assay 10 μM 4 h causes ER-stress response over the p-eIF2α branch, but does not induce CHOP? 24686080
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
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
A549 Function assay 1 to 10 uM 24 hrs Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method 24012124
Jurkat Antiproliferative assay 1 to 3 days Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50 = 4.5 μM. 23711832
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50 = 5.2 μM. 22339433
K562 Antiproliferative assay 4 days Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50 = 5.3 μM. 21174434
A375 Antiproliferative assay 4 days Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50 = 3.9 μM. 21174434
H1299 Antiproliferative assay 4 days Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50 = 2.4 μM. 21174434
PC3 Antiproliferative assay 4 days Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50 = 2.1 μM. 21174434
HDMEC Kinase Assay 0.25/0.5/1 μM 24 h reduces CK2 kinase activity, vWF expression and secretion 26381437
platelets Kinase Assay 1/5/10 μM 0.5 h reduces CK2 kinase activity and platelet aggregation 26381437
UM-SCC1 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=4.1 μM 25798061
H1299 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
H358 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
Calu-1? Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H1299 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H28 Growth Inhibition Assay 0.01-30 μM 72 h IC50=7.2 μM 25422081
A431? Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
R-LAMA84 Function Assay 3?μM 24 h reduces CK2 activity 24012109
S-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h inhibits cell growth concentration dependently 24012109
R-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h inhibits cell growth concentration dependently 24012109
Nalm6? Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
HCT116? Apoptosis Assay 10 μM 24/48 h induces apoptosis 24686080
MDA-MB-231 Function Assay 2/5/10 μM 4 h decreases the constitutive phosphorylation of both p-S529-p65 and p-S129-Akt 25153725
MDA-MB-231 Function Assay 2/5/10 μM 4 h inhibits serine 529 phosphorylation and the expression of IL-6, IL-8 25153725
U87-MG Growth Inhibition Assay 1/5/10 μM 24/48/72 h inhibits cell growth both concentration and time dependently 25241897
UM-SCC-1 Clonogenic Assay 0.5-5 μM 14 d ?inhibits clonogenic survival and sphere formation 25379016
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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
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生物活性

產(chǎn)品描述 Silmitasertib (CX-4945)是有效的，選擇性CK2(casein kinase 2)抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為1 nM,對(duì) Flt3, Pim1 和 CDK1作用效果稍弱(細(xì)胞試驗(yàn)中沒有活性)。Silmitasertib可誘導(dǎo)自噬并促進(jìn)細(xì)胞凋亡。Phase 1/2。
特性 CX-4945是促進(jìn)人類臨床實(shí)驗(yàn)的CK2的第一個(gè)口服生物相容性小分子抑制劑。
靶點(diǎn)
CK2 [1]
(Cell-free assay)
1 nM
體外研究(In Vitro)
體外研究活性

CX-4945是CK2特異的抑制劑，它只抑制238種激酶中的7種并且在0.5 μM濃度時(shí)它的抑制率超過(guò)90%，這是CK2的IC50的500多倍。雖然在無(wú)細(xì)胞系統(tǒng)中CX-4945抑制FLT3, PIM1和CDK1的IC50分別為35 nM, 46 nM和56 nM，但是在細(xì)胞基礎(chǔ)上的功能實(shí)驗(yàn)中10 μM的CX-4945對(duì)FLT3, PIM1和 CDK1抑制作用不強(qiáng)。CX-4945有廣譜的抗惡性細(xì)胞增生活性。乳腺癌細(xì)胞系對(duì)CX-4945敏感性最廣泛，其EC50為1.71-20.01 μM。CX-4945的抗惡性細(xì)胞增生活性與CK2α mRNA和蛋白水平對(duì)應(yīng)，但是與CK2α'催化亞基、調(diào)整CK2β亞族和PI3K/Akt 或 PTEN突變狀態(tài)無(wú)關(guān)。CX-4945通過(guò)抑制CK2直接阻斷Akt第129位絲氨酸的磷酸化作用來(lái)抑制PI3K/Akt信號(hào)通路，而不是通過(guò)抑制激活的PTEN起作用。用CX-4945處理可以引起磷酸化p21 (T145)減少，而p21和p27整體水平則會(huì)升高，同時(shí)誘導(dǎo)caspase 3/7活性。用CX-4945處理會(huì)誘導(dǎo)BT-474細(xì)胞阻斷在細(xì)胞周期的G2/M期和BxPC-3細(xì)胞阻斷在G1期。CX-4945會(huì)抑制HUVEC的增殖、遷移及血管新生，其IC50分別是5.5 μM, 2 μM和4 μM。在含氧量低的情況下BT-474和BxPC-3細(xì)胞用CX-4945處理，能阻斷p53和pVHL下調(diào)，降低HIF-1α的轉(zhuǎn)錄活性[1]。在Jurkat細(xì)胞中CX-4945能有效抑制內(nèi)源細(xì)胞內(nèi)的內(nèi)源CK2的活性，其IC50是0.1 μM [2]。
激酶實(shí)驗(yàn) CK2激酶實(shí)驗(yàn)
將10 μL稀釋緩沖液(ADB; 20 mM MOPS, pH 7.2, 25 mM β-磷酸甘油, 5 mM EGTA, 1 mM原釩酸鈉和 1 mM 二硫蘇糖醇)，10 μL多肽底物(RRRDDDSDDD, 溶于ADB，濃度1mM)和10 μL重組的人源CK2(ααββ-全酶, 25 ng溶于ADB)混合，加入10 μL CX-4945。加入10μLATP溶液(90% 75 mM MgCl 2, 75 μM ATP (終濃度15 μM)溶于ADB; 10% [γ-33P]ATP (儲(chǔ)存1 mCi/100 μL; 3000 Ci/mM起始反應(yīng)，30 ℃反應(yīng)10分鐘。用100 μL的0.75%的磷酸終止反應(yīng)，然后轉(zhuǎn)移到磷酸纖維素濾板上過(guò)濾。每個(gè)孔用0.75%磷酸洗5次，真空抽干5分鐘，再每孔加入15 μL閃爍液，然后用Wallac熒光計(jì)數(shù)器檢測(cè)殘留的放射性。通過(guò)對(duì)0.0001 μM 到1 μM的8個(gè)濃度的CX-4945實(shí)驗(yàn)結(jié)果的檢測(cè)，計(jì)算出IC50。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 SKBr3, MDA-MB-453, BT-474, ZR-75-1, MDA-MB-231, MDA-MB-468, T47D, MCF 7, Hs578T, MDA-MB-361, UACC-812, 等等
濃度 溶于 DMSO, 終濃度 ~100 μM
孵育時(shí)間 4 天
方法

在用藥處理前，在合適的培養(yǎng)基中按每孔3000個(gè)細(xì)胞的濃度接種細(xì)胞培養(yǎng)24小時(shí)，然后用不同濃度的CX-4945處理細(xì)胞。接種懸浮細(xì)胞并處理相同的天數(shù)。接著孵育4天，加入Alamar Blue (20 μL, 體積比每孔10%)，然后于37℃孵育4-5小時(shí)。檢測(cè)熒光，激發(fā)光為530-560 nm，放射光為590 nm。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6 p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail 30683840
Immunofluorescence β-catenin E-cadherin / Vimentin 24023938
Growth inhibition assay Cell viability 30316146
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在BT-474模型中，一天兩次口服25 mg/kg或75 mg/kg的CX-4945，具有強(qiáng)效的抗癌活性，TGI分別為88% 和97%，每組實(shí)驗(yàn)動(dòng)物9只中有2只其腫瘤的體積大小比初期的要減少50%。在BxPC-3模型中，一天兩次用75 mg/kg的CX-4945處理，TGI為93%，在治療期結(jié)束時(shí)，有3只動(dòng)物沒發(fā)現(xiàn)還有殘留的腫瘤[1]。在PC3異種移植的模型中，用25 mg/kg, 50 mg/kg或 75 mg/kg的CX-4945處理，能抑制腫瘤生長(zhǎng)，TGI分別為19%, 40%和86%[2]
動(dòng)物實(shí)驗(yàn) Animal Models 注射了BxPC-3 或BT-474細(xì)胞的免疫缺陷的雌鼠
Dosages 25或75 mg/kg
Administration 每日兩次口服
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05817708 Completed
COVID-19
Senhwa Biosciences Inc.
 November 7 2022 Phase 1
NCT04668209 Terminated
Coronavirus
University of Arizona|Senhwa Biosciences Inc.
 January 21 2021 Phase 2
NCT04663737 Completed
Covid19
Chris Recknor MD|Senhwa Biosciences Inc.
 December 3 2020 Phase 2
NCT03904862 Suspended
Medulloblastoma Childhood
Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)|American Lebanese Syrian Associated Charities (ALSAC)
 July 25 2019 Phase 1|Phase 2
NCT02128282 Completed
Cholangiocarcinoma
Senhwa Biosciences Inc.
 June 2014 Phase 1|Phase 2

化學(xué)信息&溶解度

分子量 349.77 分子式

C19H12ClN3O2
CAS號(hào) 1009820-21-6 SDF Download Silmitasertib (CX-4945) SDF
Smiles C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 70 mg/mL ( (200.13 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)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(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)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(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(wèn)題及建議解決方法

問(wèn)題 1:
How to reconstitute the compound (S2248) for in vivo uses?

回答：
For injection, CX-4945 can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml clearly. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm the solution in water bath at about 45-50℃. Then add PEG and Tween. After they mixed well, dilute with water. For oral gavage, CX-4945 can be dissolved in 1% CMC Na at 30mg/ml as a homogeneous suspension. This is a common formulation for oral gavage, and is convenience to prepare.

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