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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1818291-27-8
- 分子式: C30H26Cl2FN3O3
- 分子量:566.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 4 nM (MDM2-p53)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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.
化学情報
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CAS 番号 1818291-27-8
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分子量 566.45
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BI-0252 関連分類
HY-100765 関連分類
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