1. Apoptosis
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    E1/E2/E3 Enzyme
  3. BI-0252

BI-0252 

目录号: HY-100765
产品使用指南

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。

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BI-0252 Chemical Structure

BI-0252 Chemical Structure

CAS No. : 1818291-27-8

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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
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
  • 摩尔计算器

  • 稀释计算器

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