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GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $2,720 | 10-14 weeks | |
50 mg | $3,580 | 10-14 weeks | |
100 mg | $4,900 | 10-14 weeks |
Description | GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity. |
Targets&IC50 | PRMT8:1.7 nM , PRMT4:1148 nM , PRMT1:3.1 nM , PRMT6:5.7 nM , PRMT3:48 nM |
In vitro | GSK3368715 ?shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types. |
In vivo | GSK3368715 markedly impacts the growth of BxPC3 xenografts across all examined doses, achieving a reduction in tumor growth of 78% and 97% for the 150 mg/kg and 300 mg/kg dose groups, respectively. |
Alias | EPZ019997 |
Molecular Weight | 366.54 |
Formula | C20H38N4O2 |
Cas No. | 1629013-22-4 |
Relative Density. | 1.018 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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