Bioactivity | SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM)[1]. |
In Vivo | SHR5428(3-30 mg/kg,口服,每天一次,持续 21 天)显示出剂量依赖性肿瘤生长抑制[1]。SHR5428(2 mg/kg,口服,一次)在小鼠、大鼠和狗等不同物种中表现出良好的药代动力学特性[1]。Pharmacokinetic Parameters of SHR5428 in mouse, rat and dog[1]. |
Name | SHR5428 |
Formula | C22H23F3N5O2P |
Molar Mass | 477.42 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Jia M, et al. Discovery of SHR5428 as a selective and noncovalent inhibitor of CDK7. Bioorg Med Chem Lett. 2023 Sep 1;93:129429. |