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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 |
|---|
| AMG-193
AMG-193 is an orally active inhibitor of the PRMT5/MTA complex for studies related to solid tumors. AMG-193 (PRMT5-IN-27) inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM. |
| AZD3470
AZD3470 is a novel PRMT5 inhibitor targeting the MTA and PRMT5 complex for studies related to hematologic tumors. |
| TNG-462
TNG-462 is an orally active PRMT5 inhibitor for investigation of MTAP-deficient and/or MTA-accumulating cancers. |
| TNG908
TNG908 is a PRMT5 inhibitor that crosses the blood-brain barrier and can be used in studies related to advanced solid tumors. |
| PRMT5-IN-20
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity. |
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