ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >TGF-beta / Smad >TGF-beta / Smad inhibitors >LY2109761


LY2109761 Suppliers list
Tel: +86 21 5161 9050/ 5187 7795
Products Intro: Product Name:LY2109761
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
Company Name: Biochempartner
Tel: 0086-13720134139
Products Intro: Product Name:LY2109761
Purity:98% HPLC LCMS Package:10G;20G
Company Name: Hubei xin bonus chemical co. LTD
Tel: 86-13657291602
Products Intro: Product Name:LY2109761
Purity:0.99 Package:5KG;1KG
Company Name: BOC Sciences
Tel: 1-631-485-4226
Products Intro: Product Name:LY2109761
Package:$550/100mg $1950/1g Remarks:LY2109761 is a novel inhibitor of TGF-β receptor type I/type II kinases (IC50 = 69 nM), displaying antitumor activity. In vivo study demonstrated that LY2109761, in combination with gemcitabine, signi
Company Name: Alchem Pharmtech,Inc.
Tel: 8485655694
Products Intro: Product Name:4-(2-((4-(2-(Pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl)oxy)ethyl)morpholine
Purity:97+% Package:1g;10g;100g;;1kg Remarks:Z-58062

Lastest Price from LY2109761 manufacturers

  • LY2109761
  • US $7.00 / KG
  • 2020-01-14
  • CAS:700874-71-1
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 1000kg
LY2109761 Basic information
Description In vitro In vivo
Product Name:LY2109761
Synonyms:LY2109761/LY-2109761;LY2109761;Quinoline, 4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-Morpholinyl)ethoxy]-;4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]quinoline;LY210976;4-[2-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]oxyethyl]Morpholine;N-CYCLOPENTYL-WEI -ALANINE;N-CYCLOPENTYL-Β-ALANINE
Product Categories:Inhibitors;Smad;TGF-beta
Mol File:700874-71-1.mol
LY2109761 Structure
LY2109761 Chemical Properties
Boiling point 640.9±55.0 °C(Predicted)
density 1.34
Safety Information
HS Code 29349990
MSDS Information
LY2109761 Usage And Synthesis
DescriptionLY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.
In vitro LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when combined with gemcitabine in combination index value of 0.36581. Blocking TβRI/II kinase activity with LY2109761 (5 μM) completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, significantly enhances the detachment-induced apoptosis by 26% at 8 hours treatment, and completely suppresses TGF-β–induced Smad2 phosphorylation. LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. LY2109761 pretreatment enhances radiosensitivity of glioblastoma cells via TGF-β signaling blockage. LY2109761 (10 μM) reduces the self-renewal and proliferation of GBM-derived cancer stem–like cells (CSLC), which can be significantly enhanced when combined with radiation.
In vivoAdministration of LY2109761 (50 mg/kg) alone or in combination with gemcitabine (25 mg/kg) significantly reduces the tumor volume by ~70% and ~90%, respectively, prolongs the survival with the median survival duration of 45.0 days and 77.5 days, respectively, and reduces spontaneous abdominal metastases in the L3.6pl/GLT Xenograft mice model. In consistent with the in vitro effect, administration of LY2109761 alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively, decreases tumor invasion and tumor microvessel density, and significantly enhances radiation-induced tumor growth delay in the U87MG xenograft mice model.
LY2109761 Preparation Products And Raw materials
Tag:LY2109761(700874-71-1) Related Product Information
SB525334 SB 431542 xav-939 GW788388 N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide LY 2157299