1. Apoptosis
  2. MDM-2/p53
  3. BI-0252

BI-0252 

Cat. No.: HY-100765
Handling Instructions

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.

For research use only. We do not sell to patients.

BI-0252 Chemical Structure

BI-0252 Chemical Structure

CAS No. : 1818291-27-8

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Description

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]

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.
Molecular Weight

566.45

Formula

C₃₀H₂₆Cl₂FN₃O₃

CAS No.

1818291-27-8

SMILES

ClC1=C(F)C([[email protected]@H]2[[email protected]@]3(C(C=CC(Cl)=C4)=C4NC3=O)N(CC5CC5)[[email protected]@H]6[[email protected]]2N[[email protected]@H](C7=CC=C(C(O)=O)C=C7)C6)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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BI-0252
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HY-100765
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