[CAS NO. 1818291-27-8] BI-0252
PRODUCTS SPECIFICATIONS [1818291-27-8]
DESCRIPTION [1818291-27-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 566.45 |
| Molecular Formula | C30H26Cl2FN3O3 |
| SMILES | ClC1=C(F)C([C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)N(CC5CC5)[C@@H]6[C@H]2N[C@@H](C7=CC=C(C(O)=O)C=C7)C6)=CC=C1 |
Summary
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]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.