All AbMole products are for research use only, cannot be used for human consumption.
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.
| 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 |
| Formulation | |
| Dosages | 75 mg/kg, 150 mg/kg, 300 mg/kg |
| Administration | Oral gavage |
| 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 |
| Related PRMTs Products |
|---|
| C7280948
C7280948 is an inhibitor of histone arginine methyltransferase PRMT1 with IC50 values of 12.75 uM. |
| EPZ015666
EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
| SGC707
SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. |
| EPZ020411
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8. |
| XY1
XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
