GSK3368715 trihydrochloride structure
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Common Name | GSK3368715 trihydrochloride | ||
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CAS Number | 2227587-26-8 | Molecular Weight | 475.92 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C20H41Cl3N4O2 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of GSK3368715 trihydrochlorideGSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1]. |
Name | GSK3368715 3HCl |
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Description | GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1]. |
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Related Catalog | |
Target |
PRMT4:1148 nM (IC50) PRMT3:48 nM (IC50) PRMT1:3.1 nM (IC50) PRMT6:5.8 nM (IC50) PRMT8:1.7 nM (IC50) |
In Vitro | GSK3368715 trihydrochloride (EPZ019997) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types[1]. |
In Vivo | GSK3368715 trihydrochloride (EPZ019997) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively[1]. |
References |
Molecular Formula | C20H41Cl3N4O2 |
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Molecular Weight | 475.92 |
Storage condition | -20°C |