BI-0252
CAS No. : 1818291-27-8
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| Cat. No. : | HY-100765 |
| M.Wt: | 566.45 |
| Formula: | C30H26Cl2FN3O3 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
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