STA-1474 sodium
STA-1474 sodium is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 sodium disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 sodium inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 sodium induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 sodium induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 sodium can be used in the research of osteosarcoma.
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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: 1402907-09-8
- 分子式: C20H19N4Na2O6P
- 分子量:488.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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HSP90 |
HSP70 |
Caspase 3 |
p-STAT3 |
Met |
Akt |
STA-1474 (0.001-1 μM; 1-7 days) sodium potently inhibits the proliferation of D17, OSA2, OSA8 and MG63 osteosarcoma cell lines, with IC50 values ranging from 0.011 μM to 0.043 μM, and exhibits selectivity for OSA cells relative to normal canine osteoblasts (IC50 = 0.072 μM)[1].
STA-1474 (0.1 μM; 24-48 h, followed by drug-free incubation for 2-6 h) sodium mediates time-dependent and reversible downregulation of p-STAT3 in MG63 and D17 osteosarcoma cell lines, which confirms that this effect directly results from HSP90 inhibition rather than non-specific toxicity[1].
STA-1474 (0.01-1 μM; 24-48 h) sodium induces dose-dependent apoptosis in OSA8 and MG63 osteosarcoma cell lines, but does not affect apoptosis in normal canine osteoblasts; it activates caspase 3/7 in a dose-dependent manner in D17 and OSA8 osteosarcoma cell lines, and induces dose-dependent PARP cleavage in D17, OSA2, OSA8 and MG63 osteosarcoma cell lines; it downregulates HSP90 client proteins (p-Met, total Met, p-Akt, total Akt, p-STAT3), and induces upregulation of stress response proteins HSP70 and HSP90[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1402907-09-8
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分子量 488.34
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分子式 C20H19N4Na2O6P
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SMILES
O=C1NN=C(N1C2=CC(C=CN3C)=C3C=C2)C4=C(O)C=C(OP(O[Na])(O[Na])=O)C(C(C)C)=C4
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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)