ChemicalBook CAS DataBase List 1818291-27-8

1818291-27-8

Name	BI-0252
CAS	1818291-27-8
Molecular Formula	C30H26Cl2FN3O3
MDL Number	MFCD32197170
Molecular Weight	566.45
MOL File	1818291-27-8.mol

Chemical Properties

Boiling point	718.3±60.0 °C(Predicted)
density	1.53±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
pka	4.21±0.10(Predicted)

Hazard Information

Description

BI-0252 is a potent, highly selective, orally active MDM2-p53 interaction inhibitor.

Uses

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].

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.

storage

Store at -20°C

References

[1] Gollner A, et al. Discovery of Novel Spiro[[3]H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction. J Med Chem. 2016 Nov 23;59(22):10147-10162. DOI:10.1021/acs.jmedchem.6b00900

Supplier

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