CG 858
Tocris Bioscience, part of Bio-Techne | Catalog # 7427
Selective BRAF-V600E protein Degrader (uSMITE™)
Key Product Details
Description
Selective BRAF-V600E protein Degrader (uSMITE™)
Product Description
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.Product Specifications
Molecular Weight
839.87
Formula
C42H39F2N7O8S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for CG 858
For research use only
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