您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Dabrafenib-d9
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Dabrafenib-d9
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dabrafenib-d9图片
CAS NO:1423119-98-5
包装:1mg
市场价:8845元

产品介绍
Dabrafenib-d9 (GSK2118436A-d9) 是氘标记的 Dabrafenib。 Dabrafenib (GSK2118436A) 是一种 ATP 竞争性 Raf 抑制剂,对 C-Raf 和 B-RafV600E 的 IC50 分别为 5 nM 和 0.6 nM。
Cas No.1423119-98-5
别名达帕菲尼杂质,GSK2118436A-d9; GSK2118436-d9
Canonical SMILESFC1=C(C2=C(C3=CC=NC(N)=N3)SC(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=N2)C=CC=C1NS(C4=C(F)C=CC=C4F)(=O)=O
分子式C23H11D9F3N5O2S2
分子量528.6
溶解度DMSO: soluble,Methanol: soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dabrafenib-d9is intended for use as an internal standard for the quantification of dabrafenib by GC- or LC-MS. Dabrafenib is an ATP-competitive inhibitor of Raf kinases (IC50s = 0.64, 0.68 and 5 nM for wild-type B-RAF kinase, mutant B-RAFV600E, and wild-type C-RAF kinase, respectively).1It also inhibits the tyrosine kinase-like kinases ALK5 and LIMK1 (IC50s = 11 and 15 nM, respectively) and the calcium/calmodulin-dependent protein kinases SIK2 and PDK2 (IC50s = 27 and 57 nM, respectively), as well as NEK11, CK1, and BRK (IC50s = 20, 41, and 79 nM, respectively) in a panel of 270 kinases at 300 nM. Dabrafenib inhibits the growth of 16 cancer cell lines expressing mutant B-RAFV600E(GI50s =<200 nm), five cell lines expressing other b-raf mutants (gi50s =<30 nm), and 19 cell lines expressing wild-type ras raf (gi50s =<7,000 nM). However, it does not inhibit the growth of four cancer cell lines expressing mutant B-RAFV600E, 133 cell lines expressing wild-type Ras and Raf, or 18 cell lines expressing mutant Ras (GI50s = >10 µM) in a panel of 195 cancer cell lines. Dabrafenib (8 nM) inhibits MAPK signaling, inhibiting phosphorylation of MEK and ERK, and activates caspase-3/7 in B-RAFV600E-expressing A375P melanoma cells but not in wild-type B-RAF-expressing human foreskin fibroblasts (EC200s =71 and >10,000 nM, respectively). It reduces tumor growth in an A375P mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg. Formulations containing dabrafenib have been used in the treatment of B-RAFV600E-expressing cancers.

1.King, A.J., Arnone, M.R., Bleam, M.R., et al.Dabrafenib; Preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesionsPLoS One8(7)e67583(2013)