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SEL120-34A 是CDK8的选择性和ATP 竞争性抑制剂,对CDK8/CycC、CDK19/CycC 和CDK9/cycT 的IC50s 为4.4 nM、10.4 nM 和1070 nM。SEL120-34A 具有抗肿瘤活性。

SEL120-34A 是CDK8的选择性和ATP 竞争性抑制剂,对CDK8/CycC、CDK19/CycC 和CDK9/cycT 的IC50s 为4.4 nM、10.4 nM 和1070 nM。SEL120-34A 具有抗肿瘤活性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 497 | In Stock | |
| 5 mg | ¥ 1,560 | In Stock | |
| 10 mg | ¥ 2,380 | In Stock | |
| 25 mg | ¥ 3,820 | In Stock | |
| 50 mg | ¥ 5,230 | In Stock | |
| 100 mg | ¥ 6,870 | In Stock |
SEL120-34A 相关产品
| 产品描述 | SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity. |
| 靶点活性 | CDK19-CyclinA:10.4 nM, CDK8-CyclinC:4.4 nM, CDK9-CyclinT:1070 nM |
| 体外活性 | SEL120-34A对CDK1、2、4、6、5、7无明显抑制作用。SEL120-34A对CDK9有较弱的抑制效果,其IC50为1070 nM。SEL120-34A对包括KG-1、SKNO-1、HEL-60、MOLM-16、OciAML-2、MV-4-11、MOLM-6和OciAML-3在内的急性髓性白血病(AML)细胞系具有活性,GI50<1 μM[1]。 |
| 体内活性 | SEL120-34A(口服剂量分别为30 mg/kg和60 mg/kg)能够抑制携带MV4-11癌细胞小鼠的肿瘤生长。SEL120-34A 在30 mg/kg的口服剂量下,可阻止KG-1衍生肿瘤的生长[1]。 |
| 分子量 | 414.14 |
| 分子式 | C15H18Br2N4 |
| CAS No. | 1609522-33-9 |
| Smiles | CC1=C2C=3N(C(=N2)N4CCNCC4)CCCC3C(Br)=C1Br |
| 密度 | 1.92 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | DMSO: 4.14 mg/mL (10 mM), Sonication is recommended. H2O: < 0.65 mg/mL (1.56mM)(insoluble) | |||||||||||||||||||||||||
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