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BI-0252
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BI-0252图片
CAS NO:1818291-27-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

BI-0252 is an orally active, selectiveMDM2-p53inhibitor with anIC50of 4 nM. BI-0252 can induce tumor regressions in allanimalsof a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers ofapoptosis[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].

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.