AMG 232 是一种有效的、选择性的、可口服的 p53-Mdm2 相互作用抑制剂，IC50值为 0.6 nM。它以 0.045 nM 的 Kd 与 Mdm2 结合。

AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.

AMG 232 (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines [1].

AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo and potently inhibits the growth of tumor xenografts in mice. It also blocks DNA synthesis and induces apoptosis in vivo[1]. AMG 232 causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg [2].

Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347, and A427 cells. Concentration: 0-10 μM [1]. Incubation Time: 72 hours.

Animal Model: Female athymic nude mice (n=10) based cancer models. Dosage: 10, 25, 75 mg/kg. Administration: Once daily by oral gavage [1].

1352066-68-2

C28H35Cl2NO5S

568.55

CS-1300;AMG232

DMSO:45mg/mL (79.15mM)
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years