BI-0252

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-0252 

BI-0252 是一种具有口服活性，选择性的 MDM2-p53 抑制剂，IC50 值为 4 nM。 BI-0252 可诱导异种移植小鼠 SJSA-1 的所有动物肿瘤消退，同时诱导肿瘤蛋白p53 (TP53) 靶基因和凋亡标志物。

BI-0252

BI-0252 Chemical Structure

CAS No. : 1818291-27-8

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生物活性

BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis[1].

IC50 & Target

IC50: 4 nM (MDM2-p53)[1]
体内研究
(In Vivo)

BI-0252 (orally; 25 mg/kg/day for 13 days and 100 mg/kg for 24 h) leads to time-dependent mRNA induction of TP53 target genes including CDKN1a, MDM2, and BBC3[1].
BI-0252 (iv and po; an iv dose of 5 mg/kg and a po dose of 50 mg/kg) showes low clearance in vivo after iv administration and high clearance after po administration. BI-0252 has high po in vivo exposure and good cellular potency[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing established subcutaneous SJSA-1 tumors[1]
Dosage: 25 mg/kg/day or a single dose of 100 mg/kg
Administration: Orally; 25 mg/kg/day for 13 days and 100 mg/kg for 24 hours
Result: Leaded to time-dependent mRNA induction of TP53 target genes.
Animal Model: Nontumor-bearing female NMRI nude mice[1]
Dosage: An iv dose of 5 mg/kg and a po dose of 50 mg/kg
Administration: Iv and po
Result: Showed low clearance in vivo after iv administration and high clearance after po administration.

分子量

566.45

Formula

C30H26Cl2FN3O3
CAS 号

1818291-27-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Gollner A, et al. Discovery of Novel Spiro[[3]H-indole-3,2′-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction. J Med Chem. 2016 Nov 23;59(22):10147-10162.

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