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Takeda-6d
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Takeda-6d图片
CAS NO:1125632-93-0
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
Takeda-6D (compound 6d) 是一种口服有效的 BRAF/VEGFR2 抑制剂,IC50 值分别为 7.0 和 2.2 nM。 Takeda-6D 通过抑制 293/KDR 和 VEGF 刺激的 HUVEC 细胞中的 VEGFR2 途径显示抗血管生成。Takeda-6D 显示对 ERK1/2 磷酸化的显着抑制。 Takeda-6D 显示出抗肿瘤活性。
Cas No.1125632-93-0
Canonical SMILESN#CC1(CC1)C2=C(Cl)C(C(N([H])C3=CC(OC4=NC5=C(C=C4)N=C(N([H])C(C6CC6)=O)S5)=CC=C3F)=O)=CC=C2
分子式C27H19ClFN5O3S
分子量548
溶解度DMSO: 20mM
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Takeda-6d is a dual inhibitor of RAF kinases and VEGFR2.1It 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-RAFV600Ewhen 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.

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)