Dabrafenib (GSK2118436), B-Raf mutant inhibitor (TBI1569)

Description

Product Details

Formal Name: N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide

Alternate Names: GSK2118436

Molecular Formula: C₂₃H₂₀F₃N₅O₂S

Formula Weight: 519.56

CAS Number: 1195765-45-7

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 30 mg/ml), or in Ethanol (up to 1 mg/ml with warming).

Storage: -20°C

Stability: ≥ 1 year.

Applications

B-Raf mutant inhibitor

Functions

Dabrafenib 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). 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. Induces epithelial differentiation in BRAF-mutant colorectal cancer cells.

Application Procedures

First dissolved in DMSO (up to 30 mg/ml), or in Ethanol (up to 1 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.