| Company Name: |
SYN|thesis med chem P/L
|
| Tel: |
+86-021-50720296 |
| Email: |
service@synkinase.com |
| Products Intro: |
Product Name:Takeda-6d
CAS:1125632-93-0
Purity:>98% Package:1Mg;5Mg;10Mg;50Mg;100Mg
|
|
| | Takeda-6d Basic information |
| Product Name: | Takeda-6d | | Synonyms: | Takeda-6d;2-Chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)aMino][1,3]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]benzaMide;TAKEDA 6D;TAKEDA6D;CS-2670;Benzamide, 2-chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)amino]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]-;antitumor,HUVEC cells,VEGFR,inhibit,antiangiogenesis,Raf,Vascular endothelial growth factor receptor,PKR-like endoplasmic reticulum kinase,orally active,Takeda-6D,Inhibitor,Takeda 6d,PERK,Takeda6d,Raf kinases,Protein kinase R-like endoplasmic reticulum kinase | | CAS: | 1125632-93-0 | | MF: | C27H19ClFN5O3S | | MW: | 547.99 | | EINECS: | | | Product Categories: | | | Mol File: | 1125632-93-0.mol |  |
| | Takeda-6d Chemical Properties |
| storage temp. | -20°C | | solubility | DMSO: 20mM | | form | A solid |
| | Takeda-6d Usage And Synthesis |
| Biological Activity | Takeda-6d is a dual inhibitor of RAF kinases and VEGFR2.1 It inhibits wild-type B-RAF, mutant B-RAFV600E, and C-RAF (IC50s = 12, 7, and 1.5 nM, respectively), as well as VEGFR2 (IC50 = 2.8 nM). Takeda-6d is selective for these kinases over a panel of 19 additional kinases (IC50s = >1,000 nM) but does inhibit FGFR3, PDGFRα, and PDGFRβ (IC50s = 22, 12, and 5.5 nM, respectively). It inhibits MEK and ERK1/2 phosphorylation in several colon cancer and melanoma cell lines expressing B-RAFV600E when used at concentrations ranging from 100 to 1,600 nM, as well as inhibits VEGF-A-induced phosphorylation of VEGFR2 in VEGFR2-overexpressing KDR cells (IC50 = 0.53 nM). Takeda-6d (10 mg/kg) reduces tumor volume in an A375 melanoma mouse xenograft model. | | References | 1.Okaniwa, M., Hirose, M., Imada, T., et al.Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffoldsJ. Med. Chem.55(7)3452-3478(2012) |
| | Takeda-6d Preparation Products And Raw materials |
|