PF-4942847
PF-4942847 is an orally active HSP90 inhibitor with an IC50 of approximately 50 nM. PF-4942847 induces apoptosis in osteosarcoma cells, increases the proportion of cells in the sub-G1 phase and PARP cleavage, reduces the expression of Akt, Erk, MYC, c-MET and STAT-3, and regulates HSP expression. PF-4942847 can be used in studies related to osteosarcoma and HSP90.
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: 1046859-34-0
- 分子式: C20H18Cl2F3N7O2
- 分子量:516.31
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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
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1299 | IC50 |
0.12 μM
Compound: 34
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Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay
Inhibition of human HSP90 in human NCI-H1299 cells assessed as Akt degradation after 24 hrs by luminex assay
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[PMID: 21438541] |
体外実験
PF-4942847 inhibits cell growth in a dose-dependent manner in osteosarcoma cell lines U2OS, SaOS2, MNNG/HOS, KHOS, MG63, G292, CAL72, SJSA1 and 143B, with an IC50 of approximately 50 nM[1].
PF-4942847 induces apoptosis in osteosarcoma cell lines including U2OS, SaOS2, MNNG/HOS, KHOS, MG63, G292, CAL72, SJSA1 and 143B, as evidenced by increased proportions of cells in the sub-G1 phase and enhanced PARP cleavage[1].
PF-04942847 decreases the expression of Akt, Erk, MYC, c-MET and STAT-3, and modulates the expression of HSP in osteosarcoma cells[1].
PF-4942847 inhibits osteoclast differentiation of purified human CD14+ monocytes, and its effect differs from that of the control HSP90 inhibitor 17-AAG[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic mice bearing MNNG/HOS osteosarcoma xenografts[1]
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Dosage:25 mg/kg
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Administration:Oral administration (p.o.); 3 times/week
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Result:Significantly inhibited tumor growth by approximately 40% and prolonged survival compared with controls.
化学情報
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CAS 番号 1046859-34-0
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分子量 516.31
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分子式 C20H18Cl2F3N7O2
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SMILES
O=C(NCC(F)(F)F)N1CC=2N=C(N=C(C=3C(Cl)=CC(Cl)=CC3OCCN4N=CC=C4)C2C1)N
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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)
PF-4942847 関連分類
HY-108336 関連分類
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