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Cat. No. Name Size Price Add Cart
KI2791Dabrafenib Mesylate5 mg$176
Dabrafenib Mesylate10 mg$220
Dabrafenib Mesylate20 mg$332
Dabrafenib Mesylate50 mg$526
Dabrafenib Mesylate100 mg$780
Dabrafenib Mesylate200 mg$1250
Dabrafenib Mesylate1 g$5000

Chemical Characteristic

Product NameDabrafenib Mesylate
CAS No.1195768-06-9
Molecular Weight 615.57
FormulaC23H20F3N5O2S2.CH4O3S
Chemical NameN-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide;methanesulfonic acid
Smilesc1(c(cccc1F)F)S(=O)(=O)Nc1c(c(ccc1)c1nc(sc1c1nc(ncc1)N)C(C)(C)C)F CS(=O)(=O)O
Chemical Structure

Biological activities

Dabrafenib mesylate is a mutant-BRAF kinase inhibitor. The IC50 of dabrafenib mesylate against BRAFV600E is 0.8 nM. Meanwhile, dabrafenib mesylate also inhibits the kinase activity of wild-type B-Raf and c-Raf with IC50s of 3.2 and 5.0 nM, respectively.[1] In vivo, dabrafenib mesylate inhibits the MAPK pathway in BRAFV600E-mutated melanoma cells leading to decreased proliferation and regression in xenograft mouse models.[2]

Protocols

In vivo, Dabrafenib mesylate is dissolved in DMSO.[2]

References

[1] Laquerre S, Arnone M, Moss K, et al. A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding B-RafV600E mutation. Mol Cancer Ther, 2009, 8 (12 Suppl 1).
[2]Hauschild A, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet. 2012, 380 (9839): 358-365.

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