CG 858

Name: CG 858
Brand: Tocris Bioscience
SKU: 7427

Tocris Bioscience, part of Bio-Techne | Catalog # 7427

COA / SDS

Selective BRAF-V600E protein Degrader (uSMITE™)

Key Product Details

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% (HPLC)
Molecular Weight:	839.87

View Full Technical Details for CG 858

Technical Data
Citations

Biological Activity for CG 858

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.

Licensing Information

Sold under license from Cullgen.

Technical Data for CG 858

M. Wt	839.87
Formula	C₄₂H₃₉F₂N₇O₈S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2417296-82-1
PubChem ID	155551346
InChi Key	AAIPPJPUZKZIHC-UHFFFAOYSA-N
Smiles	CCCS(=O)(NC1=CC=C(C(C(C2=CNC3=NC=C(C4=CC=C(C=C4)CNC(CCCCNC5=CC=C6C(N(C(C6=C5)=O)C7CCC(NC7=O)=O)=O)=O)C=C23)=O)=C1F)F)=O

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.

Solubility for CG 858

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	83.99	100

Preparing Stock Solutions for CG 858

The following data is based on the product molecular weight 839.87.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.19 mL	5.95 mL	11.91 mL
5 mM	0.24 mL	1.19 mL	2.38 mL
10 mM	0.12 mL	0.60 mL	1.19 mL
50 mM	0.02 mL	0.12 mL	0.24 mL

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References for CG 858

References are publications that support the biological activity of the product.

Han Discovery of selective small molecule degraders of BRAF-V600E. J.Med.Chem. 2020 PMID: 32223235