CG 858
Chemical Name: N-[[4-[3-[2,6-Difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]pentanamide
Purity: ≥98%
Biological Activity
CG 858 is a selective BRAF-V600E protein Degrader (uSMITE™). CG 858 comprises the BRAF kinase inhibitor vemurafenib linked to the E3 ligase ligand Thalidomide (Cat. No. 0652). CG 858 dose-dependently degrades BRAF-V600E but not wild type BRAF, and reduces cell viability and colony formation in HT-29 and A375 cells (DC50 values are 124 nM and 500 nM, respectively). Exhibits 88% degradation at 500 nM. CG 858 also impairs melanoma cell growth.CG 858 negative control (Cat. No. 7428) and B-Raf antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3424.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
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