SEL120-34A

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

SEL120-34A 是一种 ATP 竞争性、选择性、口服活性 CDK8 抑制剂，可抑制 CDK8/CycC 和 CDK19/CycC 复合物的激酶活性，IC50 分别为 4.4 nM 和 10.4 nM。

SEL120-34A is an ATP-competitive, selective, orally active CDK8 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively; shows no significant inhibition on other members of the CDK family (200-fold over CDK9); inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells, inhibits IFN- responsive genes expression in vitro; exhibits complete inhibitions of STAT1 S727 and STAT5 S726 in Colo-205 CRC xenograft tissues in mice (60mg/kg).

SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726.

SEL120-34A (30, 60 mg/kg, p.o.) inhibits the growth of tumor in mice bearing MV4-11 cancer cells, and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration.

SEL 120-34A

Angiogenesis

CDK

CDK

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1609522-33-9

414.145

C15H18Br2N4

>98% (HPLC)

——

CC1=C2C3=C(CCCN3C(=N2)N4CCNCC4)C(=C1Br)Br

7,8-Dibromo-9-methyl-2-piperazin-1-yl-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline

(-20℃)

With Ice Pack

≥ 2 years