Raf Degrader

Tagarafdeg (CFT1946) is an orally active, blood-brain barrier-penetrant, and selective bifunctional BiDAC degrader of the BRAF^V600E/K mutant protein, with a DC₅₀ of 14 nM in A375 cells. Tagarafdeg mediates the ubiquitination and proteasomal degradation of BRAF mutant proteins. Tagarafdeg inhibits tumor progression in multiple models of BRAF^V600E-mutant intracranial tumors, melanoma, and colorectal cancer. Tagarafdeg is applicable to tumor-related research.

MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma.

SJF-0628 is a PROTAC degrader of BRAF mutants, with a DC₅₀ of 6.8 nM against BRAF^V600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast cancer.

PROTAC BRAF-V600E degrader-1 is a BRAF-V600E-selective PROTAC degrader and inhibitor. PROTAC BRAF-V600E degrader-1 induces degradation of BRAF-V600E via the cellular ubiquitin proteasome system, sparing wild-type BRAF. PROTAC BRAF-V600E degrader-1 suppresses the MEK/ERK kinase cascade in melanoma cells. PROTAC BRAF-V600E degrader-1 impairs growth of melanoma cells in culture. PROTAC BRAF-V600E degrader-1 can be used for the research of melanoma, colon cancer.

PROTAC B-Raf degrader 1 is a PROTAC degrader targeting B-Raf, which recruits the ubiquitin-proteasome system to accelerate B-Raf degradation and reduce the expression of downstream Mcl-1. PROTAC B-Raf degrader 1 inhibits cancer cell proliferation, arrests cell cycle and induces apoptosis. PROTAC B-Raf degrader 1 can be used in breast cancer-related research.

CST905 is a potent BRAF-V600E PROTAC degrader with a DC₅₀ of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma.

CRBN ligand-186 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.

PROTAC B-Raf degrader 1 (Standard) is the analytical standard of PROTAC B-Raf degrader 1 (HY-111758). This product is intended for research and analytical applications. PROTAC B-Raf degrader 1 is a PROTAC degrader targeting B-Raf, which recruits the ubiquitin-proteasome system to accelerate B-Raf degradation and reduce the expression of downstream Mcl-1. PROTAC B-Raf degrader 1 inhibits cancer cell proliferation, arrests cell cycle and induces apoptosis. PROTAC B-Raf degrader 1 can be used in breast cancer-related research.