SCH529074 是 p53 的选择性激活剂 (Ki = 1 μM)，可用于非小细胞肺癌的研究。 SCH529074 恢复突变 p53 功能并中断 HDM2 介导的野生型 p53 泛素化。

SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53.

SCH529074 (2-4 μM) reduces cell viability and decreases to 20-25% in p53 mutant cells including H157, H1975, and H322, and to 68% in the p53 WT cell line A549 at 4 μM. SCH 529074 (2-4 μM) induces NSCLC cells including H157, A549, HCT116, and HCT116 p53-/- arrested at the G0/G1 phase (59%; 72%; 66%; and 57%)[2].

In female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells, SCH529074 (orally; 30 and 50 mg/kg) reduces 79 and 43% of tumor growth with the plasma exposure of 0.26–0.55 μm at 30 mg/kg and 0.39-0.79 μm at 50 mg/kg[1].

922150-11-6

C31H36Cl2N6

563.56

SCH 529074

Ethanol:33 mg/mL
DMF:33 mg/mL
DMSO:25 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years