Chemical Structure : TAK-632
CAS No.:
Catalog No.: PC-72530Not For Human Use, Lab Use Only.
TAK-632 (TAK632) is a potent, selective pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E and BRAF WT, respectively.
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TAK-632 (TAK632) is a potent, selective pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E and BRAF WT, respectively.
TAK-632 suppresses RAF activity in BRAF wild-type cells with minimal RAF paradoxical activation.
TAK-632 induces RAF dimerization but inhibits the kinase activity of the RAF dimer.
TAK-632 demonstrates potent antiproliferative effects both on NRAS-mutated melanoma cells and BRAF-mutated melanoma cells with acquired resistance to BRAF inhibitors through NRAS mutation or BRAF truncation.
TAK-632 exhibits synergistic antiproliferative effects combined with MEK inhibitor TAK-733.
TAK-632 also is a selective RIPK3 inhibitor (RIPK3 Kd =81 nM), > 60-fold selectivity against RIPK3 than RIPK1.
M.Wt | 554.520 | |
Formula | C27H18F4N4O3S | |
Appearance | Solid | |
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1. Nakamura A, et al. Cancer Res. 2013 Dec 1;73(23):7043-55.
2. Grasso M, et al. J Med Chem. 2018 Jun 14;61(11):5034-5046.
3. Chen X, et al. Br J Pharmacol. 2019 Jun;176(12):2095-2108.
4. Abt ER, et al. Cell Chem Biol. 2020 Feb 20;27(2):197-205.e6.
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