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ChemicalBook--->CAS DataBase List--->1616392-22-3

1616392-22-3

1616392-22-3 Structure

1616392-22-3 Structure
IdentificationBack Directory
[Name]

6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1,2,3,4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamide
[CAS]

1616392-22-3
[Synonyms]

GSK3326595
EPZ-015938
GSK-3326595,EPZ-015938
EPZ-015938 (GSK3326595)
EPZ015938; EPZ 015938; EPZ-015938
6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1
4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamid
4-Pyrimidinecarboxamide, 6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-
6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1,2,3,4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamide
EPZ015938; 6-[(1-ACETYLPIPERIDIN-4-YL)AMINO]-N-[(2S)-2-HYDROXY-3-(1;2;3;4-TETRAHYDROISOQUINOLIN-2-YL)PROPYL]PYRIMIDINE-4-CARBOXAMID
[Molecular Formula]

C24H32N6O3
[MDL Number]

MFCD29991177
[MOL File]

1616392-22-3.mol
[Molecular Weight]

452.55
Chemical PropertiesBack Directory
[Boiling point ]

760.3±60.0 °C(Predicted)
[density ]

1.275±0.06 g/cm3(Predicted)
[storage temp. ]

Keep in dark place,Inert atmosphere,2-8°C
[solubility ]

Soluble in DMSO (up to 20 mg/ml).
[form ]

solid
[pka]

12.44±0.46(Predicted)
[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.
Hazard InformationBack Directory
[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.
[storage]

Store at -20°C
[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
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