| CAS NO: | 1609452-30-3 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 1609452-30-3 |
| Canonical SMILES | CC1=C(Br)C(Br)=C2C3=C1N=C(N4CCNCC4)N3CCC2.[x HCl] |
| 分子式 | C15H18Br2N4.xHCl |
| 溶解度 | DMSO : 62.5 mg/mL |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SEL120-34A HCl 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 HCl 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 HCl shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A HCl 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. |
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