Home>>Signaling Pathways>> MAPK Signaling>> Raf>>Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436) Sale

(Synonyms: 达拉非尼; GSK2118436A; GSK2118436) 目录号 : GC15187

A Raf kinase inhibitor

Dabrafenib (GSK2118436) Chemical Structure

Cas No.:1195765-45-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥431.00
现货
10mg
¥525.00
现货
50mg
¥1,040.00
现货
100mg
¥1,743.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1, 2]:

Cell lines

B-RafV600E-driven melanoma lines, SKMEL28 and A375P F11, and colorectal carcinoma cells Colo205, HT29 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM for 24 h

Applications

Dabrafenib effectively inhibited cell proliferation of B-RafV600E-driven melanoma lines, SKMEL28 and A375P F11 (IC50 = 3 and 8 nM, respectively), and colorectal carcinoma cells Colo205 (IC50 = 7 nM). Moreover, dabrafenib selectively inhibited RIP3 and inhibited RIP3-mediated necroptosis for HT29 cells.

Animal experiment [1, 2]:

Animal models

CD1 nu/nu mice bearing A375P F11 (B-RafV600E) tumors model

Dosage form

0.1, 1, 10, and 100 mg/kg, oral administration, once daily for 14 days or 300 mg/kg, 100 mg/kg dabrafenib (p.o.).

Applications

Dabrafenib dose-dependently inhibited tumor growth and reduced pERK levels in A375P F11 (B-RafV600E) human melanoma tissue in vivo. Additionally, dabrafenib alleviated acetaminophen-induced liver injury in mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Rheault, T. R., Stellwagen, J. C., Adjabeng, G. M., Hornberger, K. R., Petrov, K. G., Waterson, A. G., Dickerson, S. H., Mook, R. A., Jr., Laquerre, S. G., King, A. J., Rossanese, O. W., Arnone, M. R., Smitheman, K. N., Kane-Carson, L. S., Han, C., Moorthy, G. S., Moss, K. G. and Uehling, D. E. (2013) Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Med Chem Lett. 4, 358-362

2. Li, J. X., Feng, J. M., Wang, Y., Li, X. H., Chen, X. X., Su, Y., Shen, Y. Y., Chen, Y., Xiong, B., Yang, C. H., Ding, J. and Miao, Z. H. (2014) The B-Raf(V600E) inhibitor dabrafenib selectively inhibits RIP3 and alleviates acetaminophen-induced liver injury. Cell Death Dis. 5, e1278

产品描述

Dabrafenib is a specific inhibitor of BRAF V600 mutants with IC50 values of 0.5nM, 0.6nM and 1.9nM against V600E, V600K and V600D, respectively [1].

BRAF plays a central role in regulating MAPK signaling pathway which regulates cell growth, division and differentiation. The V600E mutation of BRAF increases the kinase activity and is involved in metastatic melanomas. Dabrafenib is an ATP-competitive and reversible inhibitor of BRAF mutants. It potently inhibits BRAFV600E, BRAFV600K and BRAFV600D with IC50 values of 0.5nM, 0.6nM and 1.9nM, respectively. Dabrafenib is currently approved by FDA and is widely used in cancer patients harboring BRAF mutations. It is reported that treatment of dabrafenib shrinks the overall size of brain metastases in patients. It also has an impressive 60% response rate for melanomas outside of the brain. Dabrafenib provides a significant survival benefit in patients with metastatic melanoma [1, 2].

References:
[1] Hong S, Hong S. Overcoming metastatic melanoma with BRAF inhibitors. Archives of pharmacal research, 2011, 34(5): 699-701.
[2] Hong D S, Vence L, Falchook G, et al. BRAF (V600) inhibitor GSK2118436 targeted inhibition of mutant BRAF in cancer patients does not impair overall immune competency. Clinical Cancer Research, 2012, 18(8): 2326-2335.

Chemical Properties

Cas No. 1195765-45-7 SDF
别名 达拉非尼; GSK2118436A; GSK2118436
化学名 N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
Canonical SMILES CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F
分子式 C23H20F3N5O2S2 分子量 519.56
溶解度 ≥ 26mg/mL in DMSO, ≥ 2.59 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.9247 mL 9.6235 mL 19.2471 mL
5 mM 0.3849 mL 1.9247 mL 3.8494 mL
10 mM 0.1925 mL 0.9624 mL 1.9247 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

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

计算

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GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置