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.
For research use only. We do not sell to patients.
- CAS No.: 1808115-35-6
- Formula: C17H25NO6S
- Molecular Weight:371.45
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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STAT3 |
GPA512 is rapidly converted into its active metabolite Galiellalactone (HY-125170) in plasma across species at 37°C[1][2].
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].
GPA512 (compound 6) inhibits the proliferation of human prostate cancer cell line DU145 after 72 h, with an IC50 value of 4.81 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GPA512 (40-400 mg/kg; p.o.; single dose) is well tolerated in male CD1 mice, with no observed toxicity[2].
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 No. 1808115-35-6
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Molecular Weight 371.45
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPA512 Related Classifications
HY-123827 Related Classifications
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