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GSK3368715 2HCl

Cat. No. M10637
GSK3368715 2HCl Structure

EPZ019997 2HCl

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Biological Activity

GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively. GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro. In vivo, GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models. GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 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.

Protocol (for reference only)
Cell Experiment
Cell lines Toledo cells, BxPC3 cells, MiaPaca-2 cells, ACHN cells, MDA-MB-468 cells, RKO cells, Panc03.27 cells, etc.
Preparation method RKO cells are seeded in a clear bottom 384 well plates andtreated with a 20-point two-fold dilution series of GSK3368715 (29,325.5 to 0.03 nM) or 0.15% DMSO. Plates are incubated for 3 days at 37℃ in 5% CO2. Cells are fixed with ice-cold methanol for 30 minutes at room temperature, washed with phosphate buffered saline (PBS), then incubated with Odyssey blocking buffer (Licor) for 1 hour at room temperature.
Concentrations 0.75 nM, 2 μM
Incubation time 30 min, 3 h - 168 h
Animal Experiment
Animal models Female NMRI nu/nu mice (NMRI-Foxn1nu) implanted with tumor fragment
Dosages 75 mg/kg, 150 mg/kg, 300 mg/kg
Administration Oral gavage
Chemical Information
Molecular Weight 439.46
Formula C20H40Cl2N4O2
CAS Number 1628925-77-8
Solubility (25°C) DMSO ≥ 100 mg/mL
Water ≥ 90 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Andrew Fedoriw, et al. Cancer Cell . Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss

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Abmole Inhibitor Catalog

Keywords: GSK3368715 2HCl, EPZ019997 2HCl supplier, PRMTs, inhibitors, activators

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