BI-0252
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.
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- CAS No.: 1818291-27-8
- Formule: C30H26Cl2FN3O3
- Masse moléculaire:566.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 4 nM (MDM2-p53)[1]
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Cell Line
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Type | Value | Description | References |
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| SJSA-1 | IC50 |
471 nM
Compound: 3; BI-0252
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Antiproliferative activity against human SJSA-1 cells expression wild type p53 incubated for 3 days by Alamar Blue dye based assay
Antiproliferative activity against human SJSA-1 cells expression wild type p53 incubated for 3 days by Alamar Blue dye based assay
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[PMID: 27775892] |
| SK-OV-3 | IC50 |
>25000 nM
Compound: 3; BI-0252
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Antiproliferative activity against human SK-OV-3 cells expression p53 mutant incubated for 3 days by Alamar Blue dye based assay
Antiproliferative activity against human SK-OV-3 cells expression p53 mutant incubated for 3 days by Alamar Blue dye based assay
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[PMID: 27775892] |
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.
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Animal Model:Nude mice bearing established subcutaneous SJSA-1 tumors[1]
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Dosage:25 mg/kg/day or a single dose of 100 mg/kg
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Administration:Orally; 25 mg/kg/day for 13 days and 100 mg/kg for 24 hours
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Result:Leaded to time-dependent mRNA induction of TP53 target genes.
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Animal Model:Nontumor-bearing female NMRI nude mice[1]
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Dosage:An iv dose of 5 mg/kg and a po dose of 50 mg/kg
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Administration:Iv and po
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Result:Showed low clearance in vivo after iv administration and high clearance after po administration.
Chemical Information
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CAS No. 1818291-27-8
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Masse moléculaire 566.45
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Formule C30H26Cl2FN3O3
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BI-0252 Related Classifications
HY-100765 Related Classifications
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