Chemical Name |
Dabrafenib (Mesylate) |
CAS Number |
1195768-06-9 |
MDL Number |
MFCD20922872 |
Molecular Formula |
C24H24F3N5O5S3 |
Molecular Weight |
615.67 |
Synonyms |
GSK2118436 Mesylate;GSK 2118436B |
Introduction of 1195768-06-9 :
Dabrafenib (Mesylate) is a novel, potent, and selective Raf kinase inhibitor, and inhibits the kinase activity of B-RafV600Eand c-Raf with IC50 values of 0.6 and 5.0 nM, respectively. IC50 & Target: IC50: 0.6 nM (BRAFV600E), 5 nM (CRAF)[4] In Vitro: Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375[1]. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6[2]. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells[3]. In Vivo: Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas[5].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.