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SEL120-34A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SEL120-34A图片
CAS NO:1609522-33-9
规格:98%
分子量:414.14
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
SEL120-34A是一种有效的,选择性的,可口服的,ATP-竞争性的CDK8抑制剂,对CDK8/CycC和CDK19/CycC的IC50值分别为4.4nM和10.4nM,具有抗肿瘤活性。
CAS:1609522-33-9
分子式:C15H18Br2N4
分子量:414.14
纯度:98%
存储:Store at -20°C

Background:

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.


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[1].


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[1].


[1]. Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795.