B-Raf Degrader

Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAF^V600E with a DC₅₀ of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF^V600E splice variant. Tagarafdeg can be used in tumor research.

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.

CST905 is a potent PROTAC degrader of BRAF-V600E with a DC₅₀ of 18 nM. CST905 is suitable for cancer research.