产品说明书

TAK-632

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Chemical Structure| 1228591-30-7 同义名 : -
CAS号 : 1228591-30-7
货号 : A288054
分子式 : C27H18F4N4O3S
纯度 : 99%+
分子量 : 554.515
MDL号 : MFCD26960965
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(189.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • B-Raf

    B-Raf, IC50:8.3 nM

  • C-Raf/Raf-1

    C-Raf, IC50:1.4 nM
描述 TAK-632 is a multi-target inhibitor, targeting PDGFRβ, FGFR3, GSK3β, CDK2, P38α, PDGFRα, TIE2, and CDK1 with IC50 values ranging between 120-790 nM. Additionally, it inhibits CHK1, IKKβ, and MEK1 within an IC50 span of 1400-1700 nM. Preincubation for 1 hour allows TAK-632 to inhibit BRAF and CRAF competitively to ATP, with low ATP concentration IC50s at 15 nM for BRAF and 8.1 nM for CRAF. At higher ATP concentrations, the inhibition IC50s for BRAF and CRAF increase to 58 nM and 62 nM, respectively. In HMVII cells, TAK-632 effectively inhibits pMEK and pERK with IC50 values of 49 nM and 50 nM, respectively[1]. In terms of antiproliferative activity, TAK-632 is potent in both A375 and SK-MEL-2 cell lines, exhibiting GI50 values between 40-190 nM in A375 cells and 190-250 nM in SK-MEL-2 cells[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
293 cells Function assay 20 mins Inhibition of N-terminal GST-tagged MEK1 (unknown origin) expressed in 293 cells using GST-ERK1(K71A) as substrate after 20 mins, IC50=3.7 μM 23906342
human A375 cells Function assay 2 h Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis, IC50=12 nM 23906342
human HMVII cells Function assay 2 h Inhibition of NRASQ61k/BRAFG469V-mutant in human HMVII cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis, IC50=49 nM 23906342
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.02mL

1.80mL

0.90mL

18.03mL

3.61mL

1.80mL
参考文献

[1]Okaniwa M, et al. 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. J Med Chem. 2013 Aug 22;56(16):6478-94.

[2]Nakamura A, et al. Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res. 2013 Oct 11.