Tocris Bioscience™ SJF 0628

Catalog No.	Quantity
74-635	5 mg

Catalog No. 74-635 Supplier Tocris Bioscience™ Supplier No. 7463/5

Description

Potent BRAF PROTAC™

SJF 0628 is a potent, high affinity and mutant-selective Degrader (PROTAC™) of BRAF, comprising a ligand for the von Hippel Lindau E3 ligase joined by a piperazine linker to the BRAF kinase inhibitor vemurafenib. SJF 0628 induces degradation of all 3 classes of BRAF mutant in BRAF-dependent cancer cells without inducing degradation of the BRAFWT protein. The product degrades mutant BRAFV600E in BRAF-driven cancer cell lines (DC50 = 6.8 nM - 28 nM). SJ 0628 inhibits phosphorylation of MEK and ERK in SK-MEL-28 cells (DC50 = 10 nM) and inhibits cell growth in mutant-BRAF driven cancer cells (EC50 = 37 nM).

SJF 0661 negative control (Cat. No. 7464) also available.

PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.

Specifications

• Chemical Name or Material: (2 S,4 R)-1-(-2-(2-(4-(4-(3-(2,6-Difluoro-3-(propylsulfonamido)benzoyl)-1 H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
• CAS: 2413035-41-1
• Quantity: 5 mg
• Target: Active Degraders
• Molecular Formula: C₅₁H₅₇F₂N₉O₇S₂
• Purity: 0.98