CG 858

Catalog # Availability Size / Price Qty
7427/5
CG 858 | CAS No. 2417296-82-1 | Active Degraders
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Description: Selective BRAF-V600E protein Degrader (uSMITE™)

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%

Product Details
Reviews

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

M.Wt:
839.87
Formula:
C42H39F2N7O8S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2417296-82-1

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

Licensing Caveats:
Sold under license from Cullgen.

Product Datasheets

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