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Dabrafenib

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产品编号 T1903Cas号 1195765-45-7
别名 达拉非尼, GSK2118436A, GSK2118436

Dabrafenib (GSK2118436A) 是一种 Raf 抑制剂,抑制 C-Raf 和 B-RafV600E (IC50=5/0.6 nM),具有 ATP 竞争性。Dabrafenib 具有抗肿瘤活性,可用于治疗 B-RafV600E 突变的黑色素瘤。

Dabrafenib

Dabrafenib

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纯度: 100%
产品编号 T1903 别名 达拉非尼, GSK2118436A, GSK2118436Cas号 1195765-45-7

Dabrafenib (GSK2118436A) 是一种 Raf 抑制剂,抑制 C-Raf 和 B-RafV600E (IC50=5/0.6 nM),具有 ATP 竞争性。Dabrafenib 具有抗肿瘤活性,可用于治疗 B-RafV600E 突变的黑色素瘤。

规格价格库存数量
5 mg¥ 541现货
10 mg¥ 697现货
25 mg¥ 995现货
50 mg¥ 1,570现货
100 mg¥ 2,459现货
200 mg¥ 3,690现货
1 mL x 10 mM (in DMSO)¥ 616现货
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产品介绍

生物活性
产品描述
Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.
靶点活性
B-Raf:5.2 nM (cell free), B-Raf (V600E):0.7 nM (cell free), C-Raf:6.3 nM (cell free)
体外活性
方法:195 种肿瘤细胞用 Dabrafenib 处理 72 h,使用 CellTiter-Glo Assay 检测细胞生长。
结果:编码 BRAFV600E 的 20 个细胞系中有 16 个对 Dabrafenib 敏感 (gIC50<200 nM)。其他 5 个突变 BRAF 细胞系中的 3 个对 Dabrafenib 敏感 (gIC50<30nM),包括 WM-115(BRAFV600D) 和 YUMAC(BRAFV600K)。152 个 RAS/RAF 野生型中的133个和所有 18 个突变 RAS 细胞系对 Dabrafenib 不敏感 (gIC50>10µM)。[1]
方法:黑色素瘤细胞株 LCP(BRAFV600R)、WM266 (BRAFV600D) 和 M257 (BRAFWT) 用 Dabrafenib (3-100 nM) 处理 72 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:与具有野生型 BRAF 的对照细胞相比,具有 BRAFV600D/R 突变的细胞系对磷酸化 ERK 表现出更快更强的抑制作用。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Dabrafenib (3-100 mg/kg,0.5% hydroxypropylmethylcellulose+0.2% Tween 80 in pH 8.0 distilled water) 灌胃给药给携带人结直肠癌肿瘤 Colo 205 (BRAFV600E) 的 CD1 nu/nu 小鼠,每天一次,持续十四天。
结果:Dabrafenib 显示出剂量依赖性的肿瘤生长抑制作用,8 只小鼠中有 4 只在 100 mg/kg 剂量下显示出部分消退。[1]
方法:为检测体内抗肿瘤活性,将 Dabrafenib (0.1-100 mg/kg,0.5% hydroxypropylmethylcellulose+0.2% Tween 80 in pH 8.0 distilled water) 灌胃给药给携带人恶性黑色素瘤 A375P F11 (BRAFV600E) 的 CD1 nu/nu 小鼠,每天一次,持续十四天。
结果:Dabrafenib 可显著减少携带 B-RafV600E 人类黑色素瘤肿瘤的小鼠的肿瘤生长。100 mg/kg 组中,50% 的治疗动物观察到肿瘤完全消退。[3]
细胞实验
A375P-F11 assay: A375P cells were plated in 96-well plates by limiting dilution and single cell-derived clones were harvested and tested for sensitivity to B-Raf inhibitors. The F11 clone was selected for future studies and was named A375P-F11. Cellular pSmad Assay to Measure Anti-TGF-β Activity: Activity of compounds was tested in a mechanistic assay in HepG2 cells. Cells were seeded in 12-well plates at a density of 500,000 cells/well and allowed to adhere overnight at 37℃/5% CO2. Media (BME+10% serum) was removed and compound in serum-free media was added to the cells for 45 minutes at 37℃/5% CO2. Cells were stimulated with 1 ng/ml TGF-β for 60 minutes. Cells were lysed in buffer (25 mM Tris-HCl ph: 7.5, 2 mM EDTA, 2 mM EGTA,1% Triton X-100, 0.1 % SDS, 50 mM sodium-β-glycerophosphate, 2 mM sodium orthovanadate, 12.5 mM sodium pyrophosphate, protease and phosphatase inhibitor cocktails) for 30 minutes, scraped, collected, clarified by centrifugation and prepared for western blots in LDS/reducing reagent. Samples were resolved on 4-12% Bis-Tris gels, transferred to PVDF, and probed for total and phospho-Smad2 using antibodies. Gels were imaged using the odyssey blot scanner and quantified. Phospho:total Smad2 ratios were determined and the IC50 was defined as the concentration of compound which decreased the phospho:total ratio by 50% [1].
动物实验
Cells were implanted in nude mice and grown as tumor xenografts. Dosing began when tumors achieved ~150-200mm^3 volume. GSK2118436 was administered by oral gavage at a dose volume of 0.2 mL/20 gram body weight in 0.5% hydroxypropylmethylcellulose and 0.2% Tween-80 in distilled water pH 8.0. Dosing was daily for duration stipulated. Results are reported as mean tumor volume for n=7-8 mice/group. Tumors were measured twice weekly with Vernier calipers, and tumor volume was estimated from two-dimensional measurements using a prolate ellipsoid equation (Tumor volume mm^3 = (length x width^2) x 0.5). Complete tumor regression was defined as a >93% decrease in an individual tumor volume for at least 1 week [1].
别名达拉非尼, GSK2118436A, GSK2118436
化学信息
分子量519.56
分子式C23H20F3N5O2S2
CAS No.1195765-45-7
SmilesCC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F
密度1.443 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.8 mg/mL (5.39 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO: 55 mg/mL (105.86 mM)
溶液配制表
1mg5mg10mg50mg
1 mM1.9247 mL9.6235 mL19.2471 mL96.2353 mL
5 mM0.3849 mL1.9247 mL3.8494 mL19.2471 mL
1mg5mg10mg50mg
10 mM0.1925 mL0.9624 mL1.9247 mL9.6235 mL
20 mM0.0962 mL0.4812 mL0.9624 mL4.8118 mL
50 mM0.0385 mL0.1925 mL0.3849 mL1.9247 mL
100 mM0.0192 mL0.0962 mL0.1925 mL0.9624 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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

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