CG 858-Neg 

CG 858-Neg (compound 13) is a negative control for Thalidomide (HY-14658)-derived PROTAC degraders, targeting BRAF and BRAF^V600E with K_i values ​​of 9.5 nM and 14.4 nM, respectively. CG 858-Neg inhibits downstream ERK phosphorylation and suppresses BRAF^V600E-driven melanoma (e.g., A375 cells, IC₅₀=492 nM) and colorectal cancer (e.g., HT-29 cells, IC₅₀=459 nM) cells. CG 858-Neg can be used in research related to melanoma and colorectal cancer^[1].

CG 858-Neg (compound 13) is unable to bind to cereblon due to partial N-methylation of the thalidomide moiety^[1].

CG 858-Neg (1-1000 nM; 16 h) does not degrade BRAF^V600E and partially suppresses downstream ERK phosphorylation; at 37-1000 nM, it can inhibit the phosphorylation of downstream p-ERK in A375 cells^[1].
CG 858-Neg (1000 nM; 7 days) inhibits colony formation of A375 cells at concentrations of 200 nM and above^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

853.89

C₄₃H₄₁F₂N₇O₈S

2417296-83-2

O=C(C1=C(F)C(NS(=O)(CCC)=O)=CC=C1F)C2=CNC3=NC=C(C4=CC=C(CNC(CCCCNC5=CC=C6C(N(C7C(N(C)C(CC7)=O)=O)C(C6=C5)=O)=O)=O)C=C4)C=C32

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Han XR, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020;63(8):4069-4080.  [Content Brief]