1808115-35-6
Chemical Structure
GPA512
- CAS No.: 1808115-35-6
- Formula:C17H25NO6S
- Molecular Weight:371.45
IUPAC Name: methyl N-acetyl-S-((2aR,2a1S,4aR,6S,7R,7aS)-2a1-hydroxy-6-methyl-1-oxodecahydroindeno[1,7-bc]furan-7-yl)-L-cysteinate
InChIKey: QXOOJZPKZHXIHX-PVYQPBGNSA-N
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]
Biological Activity: 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[1][2].
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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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References
- [1]. Hellsten R, et al. Abstract C179: Preclinical characterization of GPA512: A prodrug of a direct STAT3 inhibitor for the treatment of prostate cancer. Mol Cancer Ther. 2015;14(12_Suppl_2):C179.
- [2]. Escobar Z, et al. Preclinical Characterization of 3β-(N-Acetyl l-cysteine methyl ester)-2aβ,3-dihydrogaliellalactone (GPA512), a Prodrug of a Direct STAT3 Inhibitor for the Treatment of Prostate Cancer. Journal of medicinal chemistry. 2016 May 26;59(10):4551-62. [Content Brief]
