Dabrafenib (GSK2118436A)

Hersteller Selleckchem
Kategorie
Typ Inhibitors;;Research Area/Oncology/Colorectal Cancer;;Research Area/Oncology/Skin Cancer;;Research Area/Neuroscience/Neural Signaling
Specific against other
Menge 10mg
ArtNr S2807-10
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Description
Dabrafenib (GSK2118436) is a potent ATP-competitive inhibitor of B-Raf, B-RafV600E and c-Raf with IC50 of 3.2 nM, 0.8 nM and 5.0 nM, respectively.
target
Raf
Targets
B-raf, B-RafV600E, c-Raf
IC50
3.2 nM, 3.2 nM, 3.2 nM, 3.2 nM, 3.2 nM, 3.2 nM
In vitro
Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-RafV600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-RafV600E. [1]
In vivo
Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. [1]
Clinical Trials
Dabrafenib is currently in phase 3 clinical trial in patients with melanoma.
Molecular Weight (MW)
519, 56
Formula
C23H20F3N5O2S2
CAS No.
1195765-45-7, 1195768-06-9 (methanesulfonic acid)
Synonyms
N/A
Solubility (25C)
DMSO 30 mg/mL, Water <1 mg/mL, Ethanol 2 mg/mL
Storage
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO
Chemical Name
N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2, 6-difluorobenzenesulfonamide
Picture ChemicalStructure Description
Dabrafenib (GSK2118436) Chemical Structure
Menge: 10mg
Lieferbar: In stock
Listenpreis: 127,00 €
Preis: 127,00 €
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