MC180295 是一种有效、选择性的CDK9抑制剂,IC50值为 5 nM。它对其选择性至少是对其他 CDK 激酶 22 倍,具有的抗肿瘤活性。
产品描述
MC180295 is a novel potent, highly selective CDK9 inhibitor (IC50: 5 nM), displays >22-fold selectivity over other CDKs.
体外活性
MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM). MC180295 (0.1 μM) demonstrates broad anti-cancer activity in vitro.
体内活性
MC180295 (20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells while not inhibiting human T cell growth in vivo.
Cas No.
2237942-08-2
分子式
C17H18N4O3S
分子量
358.42
别名
(rel)-MC180295;MC180295
储存和溶解度
DMSO:70 mg/mL (195.31 mM )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years