Dabrafenib Mesylate

For research use only. Not for use in humans.

目录号:S5069 别名: GSK2118436 Mesylate 中文名称:达帕菲尼甲磺酸盐

Dabrafenib Mesylate Chemical Structure

CAS No. 1195768-06-9

Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.7 nM, 5.2 nM and 6.3 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.

规格 价格 库存 购买数量  
RMB 795.3 现货
有超大折扣

今日订购,明日送达,全国免运费!

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

客户使用Selleck生产的Dabrafenib Mesylate发表文献53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 Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.7 nM, 5.2 nM and 6.3 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.
靶点
B-Raf (V600E) [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
C-Raf [1]
(Cell-free assay)
0.7 nM 5.2 nM 6.3 nM
体外研究

Dabrafenib displayed compelling inhibitory activity in enzyme and cellular mechanistic assays, and in cell proliferation assays in B-RafV600E-driven melanoma lines, SKMEL28 and A375P F11 (IC50 = 3 and 8 nM, respectively), and colorectal carcinoma line Colo205 (IC50 = 7 nM). Dabrafenib has a minimal effect in vitro on cells with wild-type B-Raf (HFF IC50 = 3.0 μM) and in tumor cells not harboring the activating B-RafV600E mutation. It is highly selective, exhibiting >500-fold selectivity for B-RafV600E compared to most kinases screened. Significant activity (<100-fold selectivity) was observed for a single kinase in the panel, Alk5. GSK2118436 is significantly less effective at inhibiting SMAD2/3 phosphorylation (IC50 = 3.7 μM) compared with inhibiting ERK phosphorylation (IC50 = 4 nM) in a cellular context[1]. Cellular inhibition of BRAFV600E kinase activity by dabrafenib resulted in decreased MEK and ERK phosphorylation and inhibition of cell proliferation through an initial G1 cell cycle arrest, followed by cell death[2].

Assay
Methods Test Index PMID
Western blot
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.

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.

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.

29167314 24735930 31158244
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 In a BRAFV600E-containing xenograft model of human melanoma, orally administered dabrafenib inhibited ERK activation, downregulated Ki67, and upregulated p27, leading to tumor growth inhibition. Dabrafenib is orally bioavailable, doesn’t significantly accumulate after multiple dosing, and causes a reduction of pERK that is sustained for up to 18 h post-dosing after 7 and 14 days of dosing[2].

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)

细胞实验:

[2]

- 合并
  • Cell lines: A375P cells
  • Concentrations: 8 nM
  • Incubation Time: 1 h
  • Method:

    A375P cells were transfected with the indicated siRNA for 72 h and treated with 8 nM dabrafenib (+) or DMSO control (−) for 1 h. Lysates were immunoblotted.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: CD1 nu/nu mice bearing A375P F11 (B-RafV600E) tumors
  • Dosages: 0.1, 1, 10, and 100 mg/kg
  • Administration: oral
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (162.42 mM)
Ethanol 5 mg/mL (8.12 mM)
Water Insoluble

* 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 615.67
化学式

C23H20F3N5O2S2.CH4O3S

CAS号 1195768-06-9
储存条件 粉状
溶于溶剂
别名 GSK2118436 Mesylate

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、SDS / 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、SDS / 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
NCT03176485 Completed Other: Solar Simulator Metastatic Cancer|Melanoma|Colon Cancer|Differentiated Thyroid Cancer|Hepatocellular Carcinoma|Renal Cell Carcinoma|Metastatic Melanoma|HCC|Metastatic Colon Cancer University of Arizona October 17 2014 Not Applicable

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
免费分装抑制剂

Raf Signaling Pathway Map

相关Raf产品

Tags: 购买Dabrafenib Mesylate | Dabrafenib Mesylate供应商 | 采购Dabrafenib Mesylate | Dabrafenib Mesylate价格 | Dabrafenib Mesylate生产 | 订购Dabrafenib Mesylate | Dabrafenib Mesylate代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID