« Back
Home /
Dabrafenib

Dabrafenib

Item no.	S2807-10mM
Manufacturer	Selleckchem
CASRN	1195765-45-7
Amount	10 mM/1 mL
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 20 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Skin Cancer Colorectal Cancer
Type	Inhibitors
Specific against	other
Smiles	CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	GSK2118436,GSK2118436A
Similar products	Dabrafenib
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	519, 56
Clinical Trials	Dabrafenib is currently in phase 3 clinical trial in patients with melanoma.
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]
Solubility (25C)	DMSO 30 mg/mL, Water <1 mg/mL, Ethanol 2 mg/mL
Information	Dabrafenib is a mutant BRAFV600E specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
Chemical Name	N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2, 6-difluorobenzenesulfonamide

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Request Data Sheet

S2807-10mM-datasheet.pdf

S2807-10mM-safety-datasheet.pdf