ChemicalBook > CAS DataBase List > GSK-3326595

GSK-3326595

Product Name: GSK-3326595
CAS No.: 1616392-22-3
Chemical Name: GSK-3326595
Synonyms: GSK3326595;6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-2-hydroxy-3-(1,2,3,4-tetrahydroisoquinolin-2-yl)propyl]pyrimidine-4-carboxamide;EPZ-015938;GSK-3326595,EPZ-015938;EPZ-015938 (GSK3326595);EPZ015938(pemrametostat);GSK3326595, 10 mM in DMSO;Pemrametostat (GSK3326595);EPZ015938; EPZ 015938; EPZ-015938;Pemrametostat (GSK3326595) ，S8664
CBNumber: CB03121890
Molecular Formula: C24H32N6O3
Formula Weight: 452.55
MOL File: 1616392-22-3.mol

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GSK-3326595 Property

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.
InChIKey: JLCCNYVTIWRPIZ-NRFANRHFSA-N
SMILES: C1=NC(NC2CCN(C(C)=O)CC2)=CC(C(NC[C@H](O)CN2CCC3=C(C2)C=CC=C3)=O)=N1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 27305
Product name: GSK3326595
Packaging: 5mg
Price: $116
Updated: 2024/03/01

Cayman Chemical

Product number: 27305
Product name: GSK3326595
Packaging: 25mg
Price: $343
Updated: 2024/03/01

Cayman Chemical

Product number: 27305
Product name: GSK3326595
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 27305
Product name: GSK3326595
Packaging: 10mg
Price: $199
Updated: 2024/03/01

ChemScene

Product number: CS-6451
Product name: GSK3326595
Purity: 99.55%
Packaging: 50mg
Price: $250
Updated: 2021/12/16

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GSK-3326595 Chemical Properties,Usage,Production

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.

in vivo

GSK3326595 (5 mg/kg, Intraperitoneal injection, three times a week for 9?weeks) increased hepatic triglyceride levels without affecting atherosclerosis in LDL receptor knockout mice^[3]. GSK3326595 (25-50 mg/kg, Oral, once a day for 2?weeks) enhances the efficacy of anti-programed cell death protein 1 (PD-1) immune checkpoint therapy (ICT) in hepatocellular carcinoma (HCC) in myelocytomatosis transgene turned on (MYC-ON) mice^[5].

Animal Model:	LDL receptor knockout mice^[3]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Did not alter atherosclerosis susceptibility. Increased hepatic triglyceride levels without changing the hyperlipidemia extent. Activated genes involved in fatty acid acquisition.

Animal Model:	myelocytomatosis transgene turned on mice^[5]
Dosage:	25 mg/kg, 50 mg/kg
Administration:	Oral
Result:	Significantly suppressed tumor growth at 50 mg/kg. Showed better therapeutic efficacy at 25 mg/kg.

IC 50

PRMT5; CDK4; CDK6

References

[1] SARAH V GERHART. Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.[J]. Scientific Reports, 2018: 9711. DOI:10.1038/s41598-018-28002-y
[2] SHATHA ABUHAMMAD. Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2019, 116 1: 17990-18000. DOI:10.1073/pnas.1901323116

GSK-3326595 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK-3326595 Suppliers

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1616392-22-3, GSK-3326595Related Search:

Diethylene glycol monomethyl ether GSK583 GSK461364 GSK547 GSK-467 GSK481 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide GSK-2256098 GSK369796 GSK2982772 MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- GSK2636771 GSK-2881078 GSK-2018682 GSK2126458 GSK484 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide RET Kinase inhibitor 1

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

GSK3326595

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

EPZ015938(pemrametostat)

6-[(1-acetyl-4-piperidyl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxy-propyl]pyrimidine-4-carboxamide

Pemrametostat, GSK3326595, EPZ015938

Pemrametostat (GSK3326595)

GSK3326595, 10 mM in DMSO

Pemrametostat (GSK3326595) ，S8664

1616392-22-3

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