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Dabrafenib(GSK2118436)
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(GSK2118436)图片
CAS NO:1195765-45-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)519.56
FormulaC23H20F3N5O2S2
CAS No.1195765-45-7(free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 30 mg/mL (57.74 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 8 mg/mL
SynonymsGSK2118436A; GSK-2118436B; GSK 2118436A; GSK2118436B (Dabrafenib Mesylate ); GSK-2118436A; GSK 2118436B. Trade name: Tafinlar.
实验参考方法
GeneralDabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice.
Animal modelA375P cells were implanted subcutaneously in female CD1 nu/nu mice and grown to form tumors [1]; Dabrafenib (orally gavage) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice [2].
FormulationDissolved in 0.5% hydroxypropylmethylcellulose, 0.2% Tween 80 in pH 8.0 distilled water
Dosages10, 30, and 100 mg/kg
AdministrationAdministered orally once daily
Reference[1] PLoS One. 2013; 8(7): e67583; [2] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.
生物活性


Dabrafenib inhibits MAPK signalling in BRAFV600E cells and is abrogated by ARAF or CRAF depletion. PLoS One. 2013; 8(7): e67583.



Modulation of pharmacodynamic markers by dabrafenib in BRAFV600E tumors.


Inhibition of BRAFV600E tumor xenograft growth by dabrafenib.