Dabrafenib-d9
(Synonyms: 达帕菲尼杂质,GSK2118436A-d9; GSK2118436-d9) 目录号 : GC47166
An internal standard for the quantification of dabrafenib
Cas No.:1423119-98-5
Sample solution is provided at 25 µL, 10mM.
Dabrafenib-d9 is 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).1 It 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 and 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)
Cas No. | 1423119-98-5 | SDF | |
别名 | 达帕菲尼杂质,GSK2118436A-d9; GSK2118436-d9 | ||
Canonical SMILES | FC1=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 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。 |
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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。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 1.8918 mL | 9.4589 mL | 18.9179 mL |
5 mM | 0.3784 mL | 1.8918 mL | 3.7836 mL |
10 mM | 0.1892 mL | 0.9459 mL | 1.8918 mL |
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 | 只 | |||
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 |
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,
体内配方配制方法:取 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 saline,混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet