Dabrafenib (GSK2118436)

目录号:S2807 别名: GSK2118436A 中文名称:达拉菲尼

仅限科研使用

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。

Dabrafenib (GSK2118436) Chemical Structure

CAS: 1195765-45-7

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
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Dabrafenib (GSK2118436)发表文献224篇:

产品安全说明书

Raf抑制剂选择性比较

相关Raf产品

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 NYHTenFZU2mwYYPlJGF{e2G7 NHTtUWQyKGh? NUDYZ5d1UW6qaXLpeIlwdiCxZjDCMXJi\iCYNkCwSUBufXSjboSgbY4hcHWvYX6gV2suVUWOLUK4JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKEWUSzDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB2IN88US=> NXn5eVZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzNpPkK0PVAxPjd|PD;hQi=>
HepG2 NIHxT|hMcW6jc3WgRZN{[Xl? MlvWTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iRWLLJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMESg{txO MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3N{c,OjR7MEC2O|M9N2F-
COLO205 M2HBTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjUWJpKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:yNFUh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlAxPyEQvF2= NWTTd3YxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzNpPkK0PVAxPjd|PD;hQi=>
HepG2 NVHBbGV2TnWwY4Tpc44hSXO|YYm= Mn3vOFUhdWmw M3;Ze2ROW09? MXzJcohq[mm2aX;uJI9nKEGua{WgbY4hXEeILXLleIEue3SrbYXsZZRm\CCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBUdWGmMjDwbI9{eGixconsZZRqd25idILlZZRm\CCob4KgOFUhdWmwczDwdolweiC2bzDUS2Yu[mW2YTDzeIlufWyjdHnvckBu\WG|dYLl[EBi\nSncjC2NEBucW6|IHL5JI9lgXO|ZYmgZoxwfCC|Y3HucoVzKGGwYXz5d4l{KHerdHigTWM2OCCxZjCzMlch|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3N{c,OjR7MEC2O|M9N2F-
HFF MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nXV|ExKM7:TR?= Mn;CO|IhcA>? NXr6Z29QTE2VTx?= NXrkUGtXUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKG:oIHj1cYFvKEiIRjDj[YxteyCqYYLic5Jqdmdid3ns[EB1gXCnIFKtVoFnKHerdHigTWM2OCCxZjCzJO69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3N{c,OjR7MEC2O|M9N2F-
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M14 M{C2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDzVXFiOTBizszN M{D5VVczKGh? M2HPemROW09? M2KxNmlEPTB;MjDuUS=> NX3VVlB[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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DU-4475 M3H2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xNEDPxE1? NVniTmhtPzJiaB?= MnTPSG1UVw>? MW\JR|UxRTVibl2= MkO3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NESwN|goRjJ|OES0NFM5RC:jPh?=
UACC-257 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzwc4kyOCEQvF2= M2fI[lczKGh? MULEUXNQ NHLxZWtKSzVyPU[gcm0> NVn2fmdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQxOzhpPkKzPFQ1ODN6PD;hQi=>
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Assay
Methods Test Index PMID
Western blot pMEK / pERK / ERK p-S6 / p-AKT308 / p-AKT473 β-catenin 31158244 24735930 29167314
Growth inhibition assay IC50 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

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04961619 Recruiting Drug: dabrafenib|Drug: trametinib Melanoma Novartis Pharmaceuticals|Novartis December 1 2021 --
NCT04547946 Recruiting Drug: dabrafenib + trametinib Malignant Melanoma Novartis Pharmaceuticals|Novartis October 15 2021 --
NCT05171374 Recruiting Drug: Dabrafenib|Drug: Trametinib Melanoma Stage III|Melanoma Stage IV|Melanoma MelanomaPRO Russia|Novartis September 30 2021 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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