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CG 858

Cat. No. 7427 Submit a Review Datasheet / COA / SDS
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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% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data for CG 858

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 0.6 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 et al (2020) Discovery of selective small molecule degraders of BRAF-V600E. J.Med.Chem. 63 4069 PMID: 32223235

If you know of a relevant reference for CG 858, please let us know.

View Related Products by Target

Keywords: CG 858, CG 858 supplier, CG858, degraders, targeted, protein, degradation, degrades, E3, ligase, uSMITE, BRAF-V600E, kinase, Ubiquitin-mediated, Small, Molecule-Induced, Target, Elimination, PROTAC, Raf, Kinase, Degraders, and, Ras, 7427, Tocris Bioscience

Citations for CG 858

Citations are publications that use Tocris products.

Currently there are no citations for CG 858. Do you know of a great paper that uses CG 858 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
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RAS Oncoproteins Scientific Review

RAS Oncoproteins Scientific Review

Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.

Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia