Crizotinib hydrochloride 是一种可口服的，具有选择性的 ATP 竞争性双ALK和c-Met抑制剂。它也是 ROS 原癌基因 1 抑制剂，可抑制肿瘤生长。在细胞的实验中，它抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化。

Crizotinib hydrochloride is a novel inhibitor of anaplastic lymphoma kinase and c-Met(IC50s of 20 and 8 nM)

Crizotinib hydrochloride(PF-2341066)potently inhibited NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells (mean IC(50) value, 24 nmol/L).?In biochemical and cellular screens, PF-2341066 was shown to be selective for c-Met and ALK at pharmacologically relevant concentrations across a panel of >120 diverse kinases.?PF-2341066 potently inhibited cell proliferation, which was associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells (IC(50) values, approximately 30 nmol/L) but not ALK-negative lymphoma cells[1].

1415560-69-8

C21H23Cl3FN5O

486.8

克里唑替尼盐酸;PF-02341066 hydrochloride

DMSO:4.9 mg/mL (10.07 mM)
H2O:50 mg/mL (102.71 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years