SCH 529074

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SCH 529074 是一种小分子突变体 p53 重激活剂，可结合 p53 DNA 结合域，Kd 为 1-2 uM。

SCH 529074 is a small molecule mutant p53 reactivator that binds p53 DNA binding domain with Kd of 1-2 uM; restores growth-suppressive function to mutant p53 and inhibits ubiquitination of p53 by HDM2.

Cell Viability Assay Cell Line:p53 mutant cells (H157, H1975 and H322) and p53 WT cell line A549Concentration:2 μM; 4 μM Incubation Time:24 hoursResult:Inhibited cancer WT and mutant cell viability.Cell Cycle Analysis Cell Line:H1975, H157, A549, HCT116, HCT116 p53-/- cells Concentration:2 μM, 4 μM, 6 μM Incubation Time:24 hours Result:Induced apoptosis in all assessed NSCLC cell lines irrespective of their p53 mutational status. Western Blot Analysis Cell Line:H1975, H322, H157, A549, HCT116, HCT116 p53-/-Concentration:2 μM, 4 μM, 6 μM Incubation Time:24 hours Result:Increased PUMA and p21 protein expression.

Animal Model:Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells Dosage:30 or 50 mg/kg Administration:Oral administration; twice daily; 4 weeks; started on day 3 until day 31 Result:Inhibited tumor growth

SCH529074

Apoptosis

MDM2-p53

MDM2-p53

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922150-11-6

563.6

C31H36Cl2N6

>98% (HPLC)

In Vitro:?DMSO : 20 mg/mL (35.49 mM)

CN(C)CCCNC1=NC(=NC2=CC=CC=C21)CN3CCN(CC3)C(C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine

(-20℃)

With Ice Pack

≥ 2 years