For research use only, not for therapeutic use.
TAK-632（Cat No.:I000893）is a potent and selective inhibitor of RAF kinases, particularly targeting BRAF, including the BRAF V600E mutant, as well as CRAF. RAF kinases are part of the MAPK/ERK signaling pathway, which plays a key role in cell proliferation, survival, and differentiation. By inhibiting RAF, TAK-632 effectively blocks downstream signaling through MEK and ERK, leading to reduced tumor cell growth and survival. It has been used in cancer research, particularly in exploring targeted therapies for cancers with dysregulated RAF/MEK/ERK signaling, such as melanoma and colorectal cancer. TAK-632 is a valuable tool for investigating RAF-related oncogenic pathways.
| Catalog Number | I000893 |
| CAS Number | 1228591-30-7 |
| Synonyms | N-[7-cyano-6-[4-fluoro-3-[[2-[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide |
| Molecular Formula | C₂₇H₁₈F₄N₄O₃S |
| Purity | ≥95% |
| Target | Raf |
| Solubility | in DMSO > 10 mM |
| Storage | Store at -20°C |
| IC50 | 2.4 nM (BRAF V600E); 1.4 nM (C-RAF); 160 nM (VEGFR) |
| IUPAC Name | N-[7-cyano-6-[4-fluoro-3-[[2-[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide |
| InChI | InChI=1S/C27H18F4N4O3S/c28-19-7-6-17(12-21(19)33-23(36)11-14-2-1-3-16(10-14)27(29,30)31)38-22-9-8-20-24(18(22)13-32)39-26(34-20)35-25(37)15-4-5-15/h1-3,6-10,12,15H,4-5,11H2,(H,33,36)(H,34,35,37) |
| InChIKey | OJFKUJDRGJSAQB-UHFFFAOYSA-N |
| SMILES | C1CC1C(=O)NC2=NC3=C(S2)C(=C(C=C3)OC4=CC(=C(C=C4)F)NC(=O)CC5=CC(=CC=C5)C(F)(F)F)C#N |
| Reference | </br>1:Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Nakamura A, Arita T, Tsuchiya S, Donelan J, Chouitar J, Carideo E, Galvin K, Okaniwa M, Ishikawa T, Yoshida S.Cancer Res. 2013 Dec 1;73(23):7043-55. doi: 10.1158/0008-5472.CAN-13-1825. Epub 2013 Oct 11. PMID: 24121489 Free Article</br>2:Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S, Tottori T, Inui Y, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T.J Med Chem. 2013 Aug 22;56(16):6478-94. doi: 10.1021/jm400778d. Epub 2013 Aug 1. PMID: 23906342 |
