Name: BI-0252
Rating: 5 (10 reviews)

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HIT ID:HIT212669459
Cas No:1818291-27-8
常用名:BI-0252
IUPAC: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]pyrrol]-5'-yl]benzoic acid
IUPAC: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]pyrrol]-5'-yl]benzoic acid
InChI key:CCPUFNJKOGKOOG-AFKAWQRRSA-N

分子式:C30H26Cl2FN3O3
分子量:566.45
氢键供体数 (HBD):3
氢键受体数 (HBA):5
LogP:3.387698
SMILES:OC(=O)c1ccc(cc1)[C@H]1C[C@H]2[C@@H](N1)[C@H](c1cccc(Cl)c1F)[C@@]1(N2CC2CC2)C(=O)Nc2cc(Cl)ccc12
SMILES:OC(=O)c1ccc(cc1)[C@H]1C[C@H]2[C@@H](N1)[C@H](c1cccc(Cl)c1F)[C@@]1(N2CC2CC2)C(=O)Nc2cc(Cl)ccc12

BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.

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