GPA512
GPA512 is an orally active STAT3 inhibitor and a prodrug of Galiellalactone (HY-125170). GPA512 inhibits the binding of STAT3 to DNA, downregulates STAT3-activated genes, and suppresses tumor growth in prostate cancer xenograft models. GPA512 is rapidly converted to Galiellalactone in plasma. GPA512 can be used in research related to castration-resistant prostate cancer.
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: 1808115-35-6
- 分子式: C17H25NO6S
- 分子量:371.45
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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
- プロトコル
- 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
IC50 & Target
[1]|
STAT3 |
体外実験
GPA512 (5 μM; monitored over 0-120 min) exhibits moderate symmetric permeability across Caco-2 cell monolayers, with no directional preference between absorptive and secretive transport[2].
GPA512 (10 μM; 2 h) is completely metabolized by mouse hepatocytes within 2 h, primarily via ester hydrolysis to form carboxylic acid (compound 3), which then spontaneously converts to Galiellalactone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
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:NMRI-nude (male)[2]
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Dosage:40 mg/kg
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Administration:p.o.; daily five times per week; 28 days
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Result:Significantly reduced tumor growth rate at day 26 and day 29.
Significantly decreased Ki67-positive cell ratio.
Significantly increased number of cleaved caspase-3-positive cells.
Significantly reduced mRNA expression of STAT3-regulated anti-apoptotic gene MCL1.
Showed non-significant decrease in BCL2 mRNA expression.
Left pSTAT3 expression unchanged in treated tumors.
Caused no weight loss, behavioral alterations, or other side effects, and all mice survived the treatment.
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Animal Model:CD1 (male, 7 weeks old, body weight 27.0-38.5 g)[2]
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Dosage:40 mg/kg; 200 mg/kg; 400 mg/kg
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Administration:p.o.; single dose
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Result:Exhibited no toxic signs, body weight shifts or pathological abnormalities across all tested doses.
化学情報
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CAS 番号 1808115-35-6
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分子量 371.45
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分子式 C17H25NO6S
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SMILES
O[C@]12[C@@]3([C@H](SC[C@@H](C(OC)=O)NC(C)=O)[C@@H](C)C[C@]1(CC[C@]2(OC3=O)[H])[H])[H]
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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)
GPA512 関連分類
HY-123827 関連分類
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