Dabrafenib

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM in cell-free assays, with 4- and 6-fold less potency against B-Raf (wt) and c-Raf, respectively. (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. 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. 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. (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.

1195765-45-7

GSK2118436

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO: 30 mg/mL (57.74 mM)

CC (C) (C) C1=NC (=C (S1) C1=NC (N) =NC=C1) C1=C (F) C (NS (=O) (=O) C2=C (F) C=CC=C2F) =CC=C1

C23H20F3N5O2S2

519.56

Storage temperature: -20°C. Stability: ≥ 2 years