Dabrafenib (GSK2118436)

For research use only. Not for use in humans.

目录号:S2807 别名: GSK2118436A 中文名称:达拉菲尼

Dabrafenib (GSK2118436) Chemical Structure

CAS No. 1195765-45-7

Dabrafenib (GSK2118436, GSK2118436A)是一种突变型BRAFV600特异性抑制剂,无细胞试验中IC50为0.7 nM,作用于B-Raf(wt)和c-Raf效果分别低7和9倍。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1481.39 现货
RMB 733.64 现货
RMB 1394.46 现货
RMB 2235.84 现货
RMB 3261.37 现货
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客户使用Selleck生产的Dabrafenib (GSK2118436)发表文献178篇:

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 Dabrafenib (GSK2118436, GSK2118436A)是一种突变型BRAFV600特异性抑制剂,无细胞试验中IC50为0.7 nM,作用于B-Raf(wt)和c-Raf效果分别低7和9倍。
靶点
B-Raf (V600E) [3]
(Cell-free assay)
B-Raf [3]
(Cell-free assay)
C-Raf [3]
(Cell-free assay)
0.7 nM 5.2 nM 6.3 nM
体外研究

Dabrafenib对Raf激酶具有选择性,对B-Raf的活性比其它测试过的91%的激酶高400倍。 Dabrafenib抑制B-RafV600E激酶,导致ERK磷酸化降低和抑制细胞的增值,在特异性编码突变的B-RafV600E的癌细胞中细胞停滞在G1期。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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SK-MEL-28 NEXBcmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3f4UlQ5KGh? MV7Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiaHHyZo9zcW6pIFLSRWYhXjZyMFWgcZV1[W62IH3lZZN2emWmIHHmeIVzKDR6IHjyd{Bz\XOjeoXybY4h[XO|YYm= M3O1S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{e0NVM4Lz5{N{e3OFE{PzxxYU6=
SK-MEL-28 NULoVWJUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXGb3BPPDhiaB?= NInhNJRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNlgh[2WubIOgbIFz[m:{aX7nJGJTSUZiVk[wNGUhdXW2YX70JJBz\WmwY4XiZZRm\CCob4KgNUBpeiCob3zsc5dm\CCkeTDpdpJi\GmjdHnvckBw\iBzLkGzJItYN21{IGXWMYxq\2i2IH\vdkA2KG2rboOgcYVie3W{ZXSgZYZ1\XJiNEigbJJ{KHKnc3H6eZJqdiCjc4PhfS=> NX7hXFh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke3O|QyOzdpPkK3O|c1OTN5PD;hQi=>
SK-MEL-28 Mo[5R5l1d3SxeHnjbZR6KGG|c3H5 MXS0PEBp M1LaUmN6fG:|dHH0bYMh[WO2aY\peJkhcW5iaIXtZY4hW0tvTVXMMVI5KGOnbHzzJIhiemKxcnnu[{BDWkGIIG[2NFBGKG23dHHueEBifCBzIHHu[EA{OCC3TTDt[YF{fXKnZDDh[pRmeiB2ODDodpMhemW|YYr1dolvKGG|c3H5 NVjxWVRqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke3O|QyOzdpPkK3O|c1OTN5PD;hQi=>
DAOY NWDMXGhwWHKrbXHyfUB{[3KnZX6gZZN{[Xl? MlTGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? NFO4W|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 M3\MXnBzcW2jcomgd4Nz\WWwIHHzd4F6 MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| M1;6N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC M3vre3BzcW2jcomgd4Nz\WWwIHHzd4F6 M37LZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NIfsfoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pMEK / pERK / ERK; 

PubMed: 31158244     


Cell lines as shown were treated with dabrafenib, over a dose range, for 1 hour. UT = untransfected.  Expression and/or phosphorylation of the indicated proteins were assessed by immunoblot.

p-S6 / p-AKT308 / p-AKT473; 

PubMed: 24735930     


Western blot analysis of phosphorylated proteins in MAPK and the PI3K-AKT pathway after 24 hours exposure to increasing concentrations of dabrafenib.

β-catenin; 

PubMed: 29167314     


HT-29 cells were treated with BRAF inhibitors Dabrafenib (2 μM), GDC-0879 (4 μM) or Vemurafenib (2 μM) for indicated times. The whole cell lysates were used for western blot with indicated antibodies.

31158244 24735930 29167314
Growth inhibition assay
IC50; 

PubMed: 24735930     


A panel of 23 BRAF(V600) mutant human melanoma cell lines was treated with serial dilutions (1-10,000 nM) of dabrafenib (A) for 72-120 hours to assess cell viability. The bars represent the average IC50 value of two or more independent experiments in duplicates and the error bars represent the SEM. 

24735930
体内研究 Dabrafenib(口服)抑制B-RafV600E突变的黑色素瘤(A375P)的生长,在免疫受损小鼠中皮下注射结肠癌(Colo205),Dabrafenib(口服)同样能抑制肿瘤生长。 [1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 30 mg/mL (57.74 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+45% PEG 300+2% Tween 80+ddH2O
5 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 519.56
化学式

C23H20F3N5O2S2

CAS号 1195765-45-7
储存条件 粉状
溶于溶剂
别名 GSK2118436A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

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 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04547946 Not yet recruiting Drug: dabrafenib + trametinib Malignant Melanoma Novartis Pharmaceuticals|Novartis January 29 2021 --
NCT04666272 Not yet recruiting Drug: dabrafenib|Drug: trametinib Melanoma Novartis Pharmaceuticals|Novartis December 22 2020 --
NCT04452877 Recruiting Drug: Dabrafenib|Drug: Trametinib Carcinoma Non-Small-Cell Lung Novartis Pharmaceuticals|Novartis August 19 2020 Phase 2
NCT04059224 Recruiting Drug: Trametinib|Drug: Dabrafenib Stage IV Melanoma|Stage III Melanoma Universitair Ziekenhuis Brussel January 28 2019 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID