BI-0252

CAS No. 1818291-27-8

BI-0252( BI 0252 | BI0252 )

Catalog No. M12794 CAS No. 1818291-27-8

A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BI-0252
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM.
  • Description
    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.
  • In Vitro
    ——
  • 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. 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.
  • Synonyms
    BI 0252 | BI0252
  • Pathway
    Apoptosis
  • Target
    MDM2-p53
  • Recptor
    MDM2-p53
  • Research Area
    Other Indications
  • Indication
    ——

Chemical Information

  • CAS Number
    1818291-27-8
  • Formula Weight
    566.45
  • Molecular Formula
    C30H26Cl2FN3O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    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
  • Chemical Name
    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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Gollner A, et al. J Med Chem. 2016 Nov 23;59(22):10147-10162.
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