Takeda-6d
- Product Name
- Takeda-6d
- CAS No.
- 1125632-93-0
- Chemical Name
- Takeda-6d
- Synonyms
- CS-2670;Takeda-6d;TAKEDA 6D;TAKEDA6D;Benzamide, 2-chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)amino]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]-;2-Chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)aMino][1,3]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]benzaMide;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
- CBNumber
- CB62642552
- Molecular Formula
- C27H19ClFN5O3S
- Formula Weight
- 547.99
- MOL File
- 1125632-93-0.mol
Takeda-6d Property
- storage temp.
- -20°C
- solubility
- DMSO: 20mM
- form
- A solid
N-Bromosuccinimide Price
- Product number
- SYN-1168-M001
- Product name
- Takeda-6d
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $211
- Updated
- 2021/12/16
- Product number
- INB0002082
- Product name
- TAKEDA-6D
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $498.94
- Updated
- 2021/12/16
- Product number
- DC10065
- Product name
- Takeda-6d
- Purity
- >98%
- Packaging
- 25mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- DC10065
- Product name
- Takeda-6d
- Purity
- >98%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
Takeda-6d Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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