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.
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- CAS. Nr.: 1808115-35-6
- Formel: C17H25NO6S
- Molecular Weight:371.45
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
STAT3 |
In Vitro
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
In Vivo
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.
Chemical Information
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CAS. Nr. 1808115-35-6
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Molecular Weight 371.45
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GPA512 Related Classifications
HY-123827 Related Classifications
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