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EPZ015666

EPZ015666 Struktur
1616391-65-1
CAS-Nr.
1616391-65-1
Englisch Name:
EPZ015666
Synonyma:
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
Summenformel:
C20H25N5O3
Molgewicht:
383.44
MOL-Datei:
1616391-65-1.mol

EPZ015666 Eigenschaften

Schmelzpunkt:
124-131°C
Siedepunkt:
686.4±55.0 °C(Predicted)
Dichte
1.331±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
Soluble in DMSO (up to 20 mg/ml)
pka
12.40±0.46(Predicted)
Aggregatzustand
powder
Farbe
white to beige
Stabilit?t:
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 Datenbank
1616391-65-1

Sicherheit

EPZ015666 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

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]

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.

EPZ015666 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


EPZ015666 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 116)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32957 60
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28172 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
Career Henan Chemica Co
+86-0371-86658258 +8613203830695
laboratory@coreychem.com China 30239 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
Changzhou Xuanming Pharmaceutical Technology Co., Ltd.
+86-519-85525359 +86-15995072465
sales@xuanmingchem.com China 914 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 22784 58
Shenzhen Shengda Pharma Limited
755-85269922 +8613424394241
sales@shengdapharm.com CHINA 310 58
Hefei Hirisun Pharmatech Co., Ltd
+8615056975894
shawn@hirisunpharm.com CHINA 9911 58

  • 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
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