ICEC 0942

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ICEC 0942 (CT7001) 是一种有效的、选择性的、口服活性的 CDK7 抑制剂，IC50 为 41 nM，选择性是 CDK2 的 15 倍 (IC50=578 nM)。

ICEC 0942 (CT7001) is a potent, selective, orally active CDK7 inhibitor with IC50 of 41 nM, displays 15-fold selectivity over CDK2 (IC50=578 nM);?displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2, CDK5 and CDK9; demonstrates sensitivity against a wide range of cancer types with GI50 values ranging between 0.2-0.3 uM; shows substantial anti-tumor effects in xenografts of both breast and colorectal cancers, also exhibits complete growth arrest of ER-positive tumor xenografts combined with tamoxifen.Solid Tumors Phase 1 Clinical.

Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment promotes cell apoptosis.Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment induces cell cycle arrest.Samuraciclib (ICEC0942; 0-10 μM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. Samuraciclib also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma.Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 μM, 0.32 μM, 0. 33 μM, 0.21 μM, 0.22 μM, 0.67 μM and 1.25 μM, respectively.:Apoptosis Analysis Cell Line:HCT116 cells Concentration:0 μM, 0.1 μM, 1 μM and 10 μM Incubation Time:24 hours Result:Induced caspase 3/7 and demonstrated PARP cleavage.Cell Cycle Analysis Cell Line:HCT116 cells Concentration:0 μM, 0.01 μM, 0.1 μM, 1 μM and 10 μM Incubation Time:24 hours Result:Showed accumulation of cells in G2/M.Western Blot Analysis Cell Line:HCT116 cells Concentration:0 μM, 0.1 μM, 1 μM and 10 μM Incubation Time:0 hour, 4 hours, 8 hours, 16 hours or 24 hours Result:PolII CTD phosphorylation was inhibited in a dose and time dependent manner in HCT116 colon cancer cells.

Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors.The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts. Animal Model:Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells.Dosage:100 mg/kg Administration:Oral gavage; daily; for 14 days Result:At day 14, tumor growth was inhibited by 60%.

ICEC0942 | CT7001

Cell Cycle/DNA Damage

CDK

CDK

Cancer

Solid Tumors

1805833-75-3

394.523

C22H30N6O

>98% (HPLC)

——

CC(C)C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCC4CCNCC4O

(3R,4R)-4-(((7-(benzylamino)-3-isopropylpyrazolo[1,5-a]pyrimidin-5-yl)amino)methyl)piperidin-3-ol

(-20℃)

With Ice Pack

≥ 2 years