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Dabrafenib | B-Raf mutant inhibitor

Dabrafenib (1195765-45-7) is a selective inhibitor of mutant B-RafV600E (IC50 = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC50 = 3.2 and 5 nM, respectively).1 Has been in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors. Endoplasmic reticulum stress and autophagy are induced in melanoma cells after treatment with dabrafenib and protect cells from dabrafenib toxicity.2 Induces epithelial differentiation in BRAF-mutant colorectal cancer cells.3

References/Citations

1) Huang et al. (2013), B-Raf and the inhibitors: from bench to bedside; J. Hematol. Oncol., 6 1
2) Ji et al. (2016), Endoplasmic reticulum stress-induced autophagy determines the susceptibility of melanoma cells to dabrafenib; Drugs Des. Dev. Ther. 10 2491
3) Herr et al. (2015), B-Raf inhibitors induce epithelial differentiation in BRAF-mutant colorectal cancer cells; Cancer Res., 75 216

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Dabrafenib | 1195765-45-7 | Structure | Supplier

Catalog#  10-1569

$34.00
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CAS:
1195765-45-7
Catalog Number:
10-1569
Activity:
B-Raf mutant inhibitor
Chemical Name:
N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide
Alternate Names:
GSK2118436
Molecular Weight:
519.56
Molecular Formula:
C23H20F3N5O2S
Solubility:
Soluble in DMSO (up to 30 mg/ml with warming), or in Ethanol (up to 1 mg/ml with warming).
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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