货号	规格	价格	上海	北京	珠海	重庆	武汉
S81252-2mg	≥98%	￥200.00 S81252-2mg ￥200.00 现货	10 10	-	-	-	-
S81252-5mg	≥98%	￥300.00 S81252-5mg ￥300.00 现货	9 9	-	-	-	-
S81252-10mg	≥98%	￥400.00 S81252-10mg ￥400.00 现货	8 8	-	-	-	-
S81252-25mg	≥98%	￥890.00 S81252-25mg ￥890.00 现货	10 10	-	-	-	-
S81252-50mg	≥98%	￥1720.00 S81252-50mg ￥1720.00 现货	12 >10	-	-	-	-
S81252-100mg	≥98%	￥2290.00 S81252-100mg ￥2290.00 2-3天	0 货期：2-3天	-	-	-	-

大包装询价收藏产品

加入购物车

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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

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

质量

浓度

体积

分子摩尔量

计算重置

TAK 632