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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-TAK-632
TAK-632

Chemical Structure : TAK-632

CAS No.: 1228591-30-7

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TAK-632 (TAK632)

货号: 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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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2480 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 554.520
分子式 C27H18F4N4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

100 mM in DMSO (55.4 mg/mL)
Chemical Name/SMILES

N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide

参考文献

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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