CFI-400437 吲哚醌衍生的、ATP 竞争性的PLK4抑制剂 (IC50值为 0.6 nM)。

CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 ( IC 50 of 0.6 nM) [1].

CFI-400437 is a potent inhibitor of MCF-7, MDA-MB-468 and MDA-MB231 cell growth [1]. CFI-400437 inhibits Aurora A, Aurora B, KDR and FLT-3 with IC 50 s of 0.37, 0.21, 0.48, and 0.18 μM, respectively, i.e. two orders of magnitude higher than its IC 50 of 0.6 nM against PLK4 [1]. CFI-400437 inhibits both AURKB and AURKC at concentrations<15 nM [2].

CFI-400437 (25 mg/kg, ip, once daily for 21 d) exhibits antitumor activity against MDA-MB-468 breast cancer mouse xenograft model [1].

1169211-37-3

C29H28N6O2

492.57

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years