CAS NO: | 1125632-93-0 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
Cas No. | 1125632-93-0 |
Canonical SMILES | N#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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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) |