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| | GSK-3326595 Basic information |
| Product Name: | GSK-3326595 | | Synonyms: | EPZ-015938;4-Pyrimidinecarboxamide, 6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-;GSK-3326595,EPZ-015938;EPZ-015938 (GSK3326595);4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamid;6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1;EPZ015938; 6-[(1-ACETYLPIPERIDIN-4-YL)AMINO]-N-[(2S)-2-HYDROXY-3-(1;2;3;4-TETRAHYDROISOQUINOLIN-2-YL)PROPYL]PYRIMIDINE-4-CARBOXAMID;EPZ015938; EPZ 015938; EPZ-015938 | | CAS: | 1616392-22-3 | | MF: | C24H32N6O3 | | MW: | 452.55 | | EINECS: | | | Product Categories: | API | | Mol File: | 1616392-22-3.mol |  |
| | GSK-3326595 Chemical Properties |
| Boiling point | 760.3±60.0 °C(Predicted) | | density | 1.275±0.06 g/cm3(Predicted) | | storage temp. | under inert gas (nitrogen or Argon) at 2–8 °C | | solubility | Soluble in DMSO (up to 20 mg/ml). | | pka | 12.44±0.46(Predicted) | | form | solid | | color | Off-white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| | GSK-3326595 Usage And Synthesis |
| Description | GSK3326595 (1616395-22-3) is a potent (IC50?= 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5.1?PRMT5 inhibition activated the p53 pathway?via?induction of alternative splicing of MDM4 leading to a potent anti-proliferative response both?in vitro?and?in vivo. Combination therapy with palbociclib (CDK4/6 inhibitor, Focus Cat.# 10-4760) and GSK3326595 lead to increased efficacy of palbociclib in treating native and resistant models of melanoma via regulation of the PRMT5-MDM4 axis.2?Currently in clinical trials.3 | | Uses | GSK-3326595 is a protein arginine methyltransferase 5(PRMT5) inhibitor under clinical trial. | | References | 1) Gerhart?et al.?(2018),?Activation of the p53-MDM4 regulatory axis defines the anti-tumor response to PRMT5 inhibition through its role in regulating cellular splicing; Sci. Rep.?8?9711
2) AbuHammad?et al.?(2019),?Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma; Proc. Natl. Acad. Sci. USA?116?179909
3) NCT02783300 |
| | GSK-3326595 Preparation Products And Raw materials |
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