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1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone

1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Struktur
1337531-89-1
CAS-Nr.
1337531-89-1
Englisch Name:
1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone
Synonyma:
PERK-IN-4;PERK Inhibitor I;GSK PERK Inhibitor;1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-fluoro-5-(trifluoromethyl)phenyl)ethanone;1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-fluoro-5-(trifluoromethyl)phenyl)ethan-1-one;1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone;Ethanone, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]-
CBNumber:
CB52620944
Summenformel:
C24H19F4N5O
Molgewicht:
469.43
MOL-Datei:
1337531-89-1.mol

1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Eigenschaften

Schmelzpunkt:
233-238°C (dec.)
storage temp. 
-20C
L?slichkeit
DMSO (Slightly), Methanol (Slightly, Heated)
Aggregatzustand
White powder
Farbe
Off-White to Pale Yellow

Sicherheit

1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften

Pale Yellow Solid

Verwenden

GSK PERK Inhibitor is an inhibitors of PERK, an important transmembrane protein of endoplasmic reticulum (ER). GSK PERK Inhibitor can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways. As a result, GSK PERK Inhibitor has potential use in the treatment of diseases such as Alzheimer's disease, stroke, Type 1 diabetes, Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung.

Enzyminhibitor

This first-in-class, orally bioavailable pyrrolopyrimidamine and smallmolecule protein kinase inhibitor (FW = 449.42 g/mol; CAS 1337531-89-1; Soluble in DMSO; Cell Permeable), also known by its code name GSK- 2606414 (or GSK2606414), its systematic name 7-methyl-5-(1-((3- trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3- d]pyrimidin-4-amine, and by many aliases, targets the protein kinase R (PKR)-like endoplasmic reticulum kinase, or PERK, IC50 = 0.4 nM, a key transducer of the unfolded protein response, or UPR. Primary Mode of Inhibition: Accumulation of unfolded proteins within the ER elicits release of ER chaperones from the stress-sensing domain of PERK. Once activated by oligomerization and autophosphorylation, PERK phosphorylates Ser-51 of eukaryotic initiation factor 2α (eIF2α), thereby inhibiting overall protein synthesis and providing time for the ER to clear itself of accumulated unfolded proteins. PERK Inhibitor I blocks ER stress-induced PERK autophosphorylation (nearly 100% inhibition at ≤30 nM after 30 min) after thapsigargin treatment (See Thapsigargin) of A549 cultures in vitro and effectively retards PxBC-3 tumor growth in mice in vivo. Other Target(s): c-Kit (IC50 = 150 nM), Aurora B (IC50 = 410 nM), BRK (IC50 = 410 nM), HRI/EIF2AK1 (IC50 = 420 nM), MLK2/MAP3K10 (IC50 = 450 nM), c-MER (IC50 = 470 nM), DDR2 (IC50 = 520 nM), PKR/EIF2AK2 (IC50 = 700 nM), and MLCK2/MYLK2 (IC50 = 700 nM), with little activity against more than 280 other kinases (IC50 >1 μM).

1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 23)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 31991 58
Hangzhou MolCore BioPharmatech Co.,Ltd.
+86-057181025280; +8617767106207
sales@molcore.com China 49734 58
J & K SCIENTIFIC LTD. 010-82848833 400-666-7788
jkinfo@jkchemical.com China 96815 76
Chemsky(shanghai)International Co.,Ltd. 021-50135380
shchemsky@sina.com China 32321 50
Shanghai TaoSu Biochemical Technology Co., Ltd. 021-33632979
info@tsbiochem.com China 8065 58
Shanghai Beckham Medical Technology Co., Ltd 021-13816613772 13816613772
huahero21@sina.com China 423 55
MQ (shanghai) Pharmaceuticals Co., Ltd. 13761635123
1014988033@qq.com China 4969 55
Shenzhen Polymeri Biochemical Technology Co., Ltd. +86-400-002-6226 +86-13028896684;
sales@rrkchem.com China 56511 58
Changzhou Xuanye Technology Co., Ltd 15195022192
279776773@qq.com China 2003 58
Energy Chemical 021-58432009 400-005-6266
marketing1@energy-chemical.com China 44808 58

  • 1-[5-(4-AMino-7-Methyl-7H-pyrrolo[2,3-d]pyriMidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoroMethyl)phenyl]ethanone
  • GSK PERK Inhibitor
  • PERK Inhibitor I
  • Ethanone, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]-
  • PERK-IN-4
  • 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-fluoro-5-(trifluoromethyl)phenyl)ethanone
  • 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-fluoro-5-(trifluoromethyl)phenyl)ethan-1-one
  • 1337531-89-1
  • Aromatics
  • Heterocycles
  • Indole Derivatives
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Aromatics, Heterocycles, Indole Derivatives, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals
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