CDKI-73 是一种具有口服活性的CDK9抑制剂，其对CDK9、CDK1 和 CDK2 的Ki值分别为 4 nM、4 nM 和 3 nM。CDKI-73 可下调 RNA 聚合酶 II 的磷酸化。CDKI-73 也是一种 Rab11 的抑制剂。

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

CDKI-73, one of the most potent CDK9 inhibitors, against a panel of AML cell lines and samples derived from 97 patients.?CDKI-73 induced cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9[3].

CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F = 56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice [1].

1421693-22-2

C15H15FN6O2S2

394.45

CDKI-73

DMSO:52 mg/mL (131.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years