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TAK-632

产品编号 T1886 CAS 1228591-30-7

TAK632 是一种有效的pan-RAF 抑制剂，对CRAF、BRAFV600E 和BRAFWT 的IC50分别为 1.4、2.4 和 8.3 nM。

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TAK-632, CAS 1228591-30-7

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	TAK-632 is a potent pan-Raf inhibitor.
靶点活性	PDGFRβ:120 nM, Aurora B:66 nM, FGFR3:280 nM, B-Raf:8.3 nM, C-Raf:1.4 nM
体外活性	在携带NRAS突变型黑素瘤的SK-MEL-2异种移植小鼠模型中,口服 TAK-632（60 or 120 mg/kg）抑制 MAPK 信号通路,抑制肿瘤的发展.
体内活性	在A375（GI50=66 nM）和HMVII系（和GI50=200 nM）中,TAK-632能够抑制细胞增殖。其中,在黑色素瘤A375细胞系(BRAFV600E)中,TAK-632抑制MEK（IC50=2 nM）和ERK磷酸化（IC50=16 nM）。在人类黑色素瘤HMVII细胞系(NRASQ61K/BRAFG469V)中,TAK-632抑制pMEK（IC50=49 nM）和pERK（IC50=50 nM）。
激酶实验	Kinase Profile Assay: Assays for serine/threonine kinases using radio labeled [γ-33P] ATP are performed in 96 well plates. BRAF and c-RAF are expressed as N-terminal FLAG-tagged protein using a baculovirus expression system. The reaction conditions are optimized for each kinase: BRAF (25 ng/well of enzyme, 1 μg/well of GST-MEK1(K96R), 0.1 μCi/well of [γ-32P] ATP, room temperature, 20 min reaction); c-RAF (25 ng/well of enzyme, 1 μg/well of GST-MEK1 (K96R), 0.1 μCi/well of [γ-32P] ATP, room temperature, 20 min reaction). Enzyme reactions are performed in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol and 0.5 μM ATP containing optimized concentration of enzyme, substrate and radiolabeled ATP as described above in a total volume of 50 μL. Prior to the kinase reaction, compound and enzyme are incubated for 5 min at reaction temperature as described above. The kinase reactions are initiated by adding ATP. After the reaction period as described above, the reactions are terminated by the addition of 10% (final concentration) trichloroacetic acid. The [γ-33P] or [γ-32P]-phosphorylated proteins are filtered in GFC filter plates with a Cell Harvester and then the plates are washed out with 3% phosphoric acid. The plates are dried, followed by the addition of 40 μL of MicroScint0. The radioactivity is counted by a TopCount scintillation counter.
细胞实验	The cells are proliferated in appropriate medium (vender recommended) supplemented with 10% heat-inactivated fetal bovine serum (FBS) and antibiotics, in tissue culture dishes placed in a humidified incubator maintained at 37°C in an atmosphere of 5% CO2 and 95% air. The anti-proliferative activity of compound is determined by treating cell lines with the compound for 3 days, followed by measurement of viable cell number in the Cell Titer-Glo assay. The cells are seeded in a 96-multiwell plate at 1500 to 4000 cells per well in medium containing FBS and cells allowed to sit down overnight. After 18–20 h, compounds at various concentrations by serial dilution are added to the cells and were cultured for 3 days in chamber. After the treatment culture, cellular proliferation is determined by a Cell Titer-Glo Luminescent Cell Viability Assay. In brief, 100 bL/well of Cell Titer-Glo Substrate solution is added to each well and the cells were cultured for an additional 10 minutes (approximately). The chemi-luminescence value is measured using a Luminescence Counter 1420 ARVO MX Light. Concentration response curves are generated by calculating the decrease in chemi-luminescence values in compound-treated samples relative to the vehicle (DMSO) treated controls. (Only for Reference)

化合物与蛋白结合的复合物	Crystal structure of human DHODH with TAK-632
分子量	554.52
分子式	C27H18F4N4O3S
CAS No.	1228591-30-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 93 mg/mL (167.7 mM)

Ethanol: 2 mg/mL (3.6 mM)

H2O: <1 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Okaniwa M, et al. J Med Chem. 2013, 56(16), 6478-6494. 2. Nakamura A, et al. Cancer Res. 2013, 73(23), 7043-7055. 3. Zhang H, Xu L, Qin X, et al. N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl) phenyl) acetamido) phenoxy) benzo [d] thiazol-2-yl) cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships and In Vivo Efficacy[J]. Journal of Medicinal Chemistry. 2019 May 28.

文献引用

1. Zhang H, Xu L, Qin X, et al. N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl) phenyl) acetamido) phenoxy) benzo [d] thiazol-2-yl) cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships and In Vivo Efficacy. Journal of Medicinal Chemistry. 2019 May 28

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TAK-632 1228591-30-7 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK Tyrosine Kinase/Adaptors PDGFR Aurora Kinase Raf FGFR inhibit TAK632 Inhibitor Raf kinases TAK 632 inhibitor

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TAK-632

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溶解度

参考文献

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剂量换算

体内实验配液计算器

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