Dabrafenib (GSK2118436)|DC Chemicals

Cas No.:	1195765-45-7
Chemical Name:	Dabrafenib
Synonyms:	Dabrafenib;Dabrafenib (GSK2118436);N-(3-(5-(2-Aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide;N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoroBenzenesulfonamide;N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide;Dabrafenib (USAN);Dabrafenib [USAN:INN];GSK 2118436;GSK-2118436;GSK2118436A;GSK-2118436A;N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzene sulfonamide;Tafinlar;UNII-QGP4HA4G1B;Dabrafenib,GSK2118436;N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide;Dabrafenib (Free Base);QGP4HA4G1B;N-{3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide;N-[3-[5-(2-aminopyrimidin-4-yl)-2-t
SMILES:	S1C(C2C([H])=C([H])N=C(N([H])[H])N=2)=C(C2C([H])=C([H])C([H])=C(C=2F)N([H])S(C2C(=C([H])C([H])=C([H])C=2F)F)(=O)=O)N=C1C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
Formula:	C₂₃H₂₀F₃N₅O₂S₂
M.Wt:	519.5624
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Dabrafenib is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
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].
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].

Cat. No.	Product name	Field of application
DC47985	GNE-9815	GNE-9815 is among the most highly kinase-selective RAF inhibitors targeting KRAS mutant cancers via combination treatment.
DC7719	ZM336372	ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.
DC7307	TAK-632	TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.
DC8791	Sorafenib free base (BAY-43-9006)	Sorafenib(BAY 43-9006) is a potent inhibitor of Raf-1 with IC50 values of 6 nM, 22 nM and 90 nM for Raf-1, B-Raf, and VEGFR2 respectively, BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro.
DC2098	Sorafenib (BAY-43-9006)	Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
DC7279	SB-590885	SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
DC9987	RAF709	RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
DC5049	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.
DC9814	PLX7904(PB04)	PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.
DC6301	PLX-4720	PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.