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• 产品描述： TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAFV600E, BRAFWT, respectively.

• 靶点： c-Raf:1.4 nM (IC50);Braf:8.3 nM (IC50);Aurora B:66 nM (IC50);PDGFRβ:120 nM (IC50);PDGFRα:610 nM (IC50);FGFR3:280 nM (IC50);TIE2:740 nM (IC50);IKKβ:3700 nM (IC50);CDK1:790 nM (IC50);CDK2:580 nM (IC50);p38α:600 nM (IC50);GSK3β:500 nM (IC50);MEK1:3700 nM (IC50);Raf; FGFR; PDGFR; AuroraKinase

• 体内研究：
  TAK-632 demonstrates dramatically improved solubility (740 μg/mL) in pH 6.8 phosphate buffer and exhibits significant oral absorption (at a dose of 25 mg/kg, AUC, 32.47 μg h/mL; F, 51.7%) in rats. In a dog PK study, 10 mg/kg administration of TAK-632 also shows superior oral bioavailability (F: 108%).Oral single administration of TAK-632 inhibits pERK in tumors at 8 h after its administration over a dose range of 1.9-24.1 mg/kg. In particular, 9.7-24.1 mg/kg dosing with TAK-632 strongly inhibits pERK levels to 11% of the control. TAK-632 exhibits dose-dependent antitumor efficacy without severe body weight reduction over a dose range of 3.9-24.1 mg/kg. Significant tumor regression is observed at 9.7 mg/kg and 24.1 mg/kg (T/C=−2.1% and −12.1%, respectively). TAK-632 exhibits potent antitumor efficacy when orally administered at 60 mg/kg once daily (T/C=37%, P<0.001) or at 120 mg/kg once daily (T/C=29%, P<0.001) for 21 days without severe toxicity in NRAS-mutant melanoma using a SK-MEL-2 xenograft model

• 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.

• 溶解性： DMSO  :  100  mg/mL  (180.34  mM;  Need  ultrasonic)

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.803 ml	9.017 ml	18.034 ml
  5 mM	0.361 ml	1.803 ml	3.607 ml
  10 mM	0.18 ml	0.902 ml	1.803 ml
  50 mM	0.036 ml	0.18 ml	0.361 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *