PLX4720, Mutant B-Raf inhibitor (TBI5113)

Description

Product Details

Formal Name: N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide

Molecular Formula: C₁₇H₁₄ClF₂N₃O₃S

Formula Weight: 413.80

CAS Number: 918505-84-7

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (30 mg/ml with warming)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Mutant B-Raf inhibitor

Functions

Potent and selective inhibitor of B-Raf, V600E mutant, IC50=13 nM (Wild type IC50=160 nM)1. It induces cell cycle arrest and apoptosis in B-RafV600E-positive cells and suppresses growth of B-RafV600E-positive xenografts. It induces tumor regression and reverses cachexia in a mouse model of human thyroid cancer harboring the B-RafV600E mutation. Early stage autophagy inhibitors and ER stress inhibition with 4-phenylbutyric acid increases the sensitivity of resistant cells to PLX4720. PLX4720 induces cytoprotective autophagy in thyroid cancer cells via AMPK-ULK1 pathway.

Application Procedures

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