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编 号：F642147
分子式：C30H26Cl2FN3O3
分子量：566.45
分子式：C30H26Cl2FN3O3
分子量：566.45
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CAS No: 1818291-27-8
产品详情
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.
体内研究：
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 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.
体内研究：
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.
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