BI-0252

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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。

CAS NO:

1818291-27-8

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.