EPZ015666

Description References

Product Name: EPZ015666
CAS No.: 1616391-65-1
Chemical Name: EPZ015666
Synonyms: CS-1657;EPZ015666;GSK3235025;GSK-3235025;EPZ015666 USP/EP/BP;EPZ-015666;EPZ 015666;GSK3235025 (EPZ015666);EPZ 015666 - GSK 3235025;EPZ-015666;EPZ 015666;GSK3235025;N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
CBNumber: CB02744609
Molecular Formula: C20H25N5O3
Formula Weight: 383.44
MOL File: 1616391-65-1.mol

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EPZ015666 Property

Melting point:: 124-131°C
Boiling point:: 686.4±55.0 °C(Predicted)
Density: 1.331±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: Soluble in DMSO (up to 20 mg/ml)
form: powder
pka: 12.40±0.46(Predicted)
color: white to beige
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
CAS DataBase Reference: 1616391-65-1

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1421
Product name: EPZ015666
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $226
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1421
Product name: EPZ015666
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $884
Updated: 2023/06/20

Cayman Chemical

Product number: 17285
Product name: EPZ015666
Purity: ≥95%
Packaging: 1mg
Price: $49
Updated: 2024/03/01

Cayman Chemical

Product number: 17285
Product name: EPZ015666
Purity: ≥95%
Packaging: 5mg
Price: $216
Updated: 2024/03/01

Cayman Chemical

Product number: 17285
Product name: EPZ015666
Purity: ≥95%
Packaging: 10mg
Price: $356
Updated: 2024/03/01

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EPZ015666 Chemical Properties,Usage,Production

Description

EPZ015666 (GSK3235025) is an orally available inhibitor of protein arginine methyltransferase-5 (PRMT5), which is involved in diverse cellular processes, including tumorigenesis, and its overexpression is observed in cell lines and primary patient samples derived from lymphomas, particularly mantle cell lymphoma (MCL).EPZ015666 showed dose-dependent antitumor activity in multiplein vitroandin vivomantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death. Therefore, it is a potential drug candidate for future cancer therapy.

References

Chan-Penebre, E, et al. "A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models." Nature Chemical Biology 11.6(2015):432.
Duncan, K. W., et al. "Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666." Acs Medicinal Chemistry Letters 7.2(2016):162-166.
http://www.sigmaaldrich.com/catalog/product/sigma/sml1421?lang=en&region=US

Description

EPZ015666 (1616391-65-1) is a selective and potent (IC50?= 22nM) inhibitor of arginine methyltransferase 5 (PRMT5).1,2?PRMT5 inhibition with EPZ015666 potently suppressed?in vivo?glioblastoma tumors3?and significantly inhibited the growth of multiple myeloma cell lines4.

Uses

Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression. PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas. Moreover, suppression of PRMT5 expression induces lymphoma cell death. EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM). It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.[Cayman Chemical]

Uses

EPZ015666 is a potent, orally bioavailable inhibitor of Protein arginine methyltransferase 5 (PRMT5). It acts by blocking the association of PRMT5 with methylosome protein 50.

Biochem/physiol Actions

EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor with an IC50 value of of 22 nM in biochemical assays and no inhibition up to the maximum tested concentration of 50 μM against a panel of 20 other protein methyltransferases. Inhibition was uncompetitive with respect to SAM. EPZ015666 showed dose-dependent antitumor activity in multiple in vitro and in vivo mantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death.

storage

Store at -20°C

References

1) Chan-Penebre?et al.?(2015),?A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models; Nat. Chem. Biol.?11?432 2) Duncan?et al.?(2015),?Structure and Property Guided Design in the Identification of PRMT5 Toll Compound EPZ015666; ACS Med. Chem. Lett.?7?162 3) Braun?et al.?(2017),?Coordinated Splicing of Regulatory Detained Introns within Oncogenic Transcripts Creates an Exploitable Vulnerability in Malignant Glioma; Cancer Cell?32?411 4) Gulia?et al.?(2018),?Protein arginine methyltransferase 5 has prognostic relevance and is a druggable target in multiple myeloma; Leukemia?32?996

EPZ015666 Preparation Products And Raw materials

Raw materials

Preparation Products

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EPZ015666 Suppliers

China 96 United Kingdom 1 United States 17 Global 114

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1616391-65-1, EPZ015666Related Search:

TYRPHOSTIN AG 879 Adapalene (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT AAL-993 EPZ004777 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide GSK-LSD1 Y27632 (hydrochloride) S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide OF-1 IMD-0354 Olaparib

EPZ015666

(S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide

GSK3235025

GSK-3235025

N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide

N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide

EPZ-015666;EPZ 015666;GSK3235025

GSK3235025 (EPZ015666)

CS-1657

EPZ-015666;EPZ 015666

EPZ 015666 - GSK 3235025

4-Pyrimidinecarboxamide, N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-

EPZ015666 USP/EP/BP

1616391-65-1

Inhibitors

API