BI-0252

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

一种有效的、高选择性的、口服活性的 MDM2-p53 相互作用抑制剂，IC50 为 4 nM。

A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM; shows in vivo efficacy in a SJSA-1 xenograft model.

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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. 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. Animal Model:Nude mice bearing established subcutaneous SJSA-1 tumors 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 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.

BI 0252 | BI0252

Apoptosis

MDM2-p53

MDM2-p53

Other Indications

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1818291-27-8

566.45

C30H26Cl2FN3O3

>98% (HPLC)

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ClC1=CC(NC([C@]23[C@@H](C4=CC=CC(Cl)=C4F)[C@H](C[C@@H](C5=CC=C(C(O)=O)C=C5)C6)[C@H]6N3CC7CC7)=O)=C2C=C1

4-[(3S,3'S,3'aS,5'R,6'aS)-6-chloro-3'-(3-chloro-2-fluorophenyl)-1'-(cyclopropylmethyl)-2-oxo-1,2,3',3'a,4',5',6',6'a-octahydro-1'H-spiro[indole-3,2'-pyrrolo[3,2-b]pyrrole]-5'-yl]benzoic acid

(-20℃)

With Ice Pack

≥ 2 years