Raf

Cat. No.

A24661

CAS No.

2364367-27-9

PROTAC B-Raf degrader 1

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf.

Cat. No.

A24708

CAS No.

2417296-84-3

PROTAC BRAF-V600E degrader-1

Synonyms: Compound 23

PROTAC BRAF-V600E degrader-1 is an effective degrader of the BRAF-V600E mutant, selectively targeting this oncogenic variant while sparing wild-type BRAF. With Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively, this compound facilitates degradation of BRAF-V600E through the ubiquitin-proteasome system (UPS). Its potent activity against melanoma cells makes it a valuable tool for research into targeted cancer therapies and mechanisms of drug resistance in BRAF-mutant tumors.

Cat. No.

A24727

CAS No.

2413035-41-1

SJF-0628

SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer.

Cat. No.

A36787

CAS No.

2417296-83-2

CG 858-Neg

CG 858-Neg is a negative control for Thalidomide-derived PROTAC degraders targeting BRAF and BRAFV600E, exhibiting Ki values of 9.5 nM and 14.4 nM, respectively. This compound effectively inhibits downstream phosphorylation of ERK and demonstrates suppression of BRAFV600E-driven tumorigenesis in melanoma (A375 cells, IC50 = 492 nM) and colorectal cancer (HT-29 cells, IC50 = 459 nM) models. CG 858-Neg is suitable for research applications focused on the mechanisms of melanoma and colorectal carcinoma.

Cat. No.

A40682

CAS No.

3002056-30-3

NST-628

NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis.

Cat. No.

A40714

CAS No.

3094183-98-6

CST905

CST905 is a highly effective PROTAC degrader specifically targeting the BRAF-V600E mutation, demonstrating a DC50 value of 18 nM. This compound facilitates the selective degradation of the BRAF-V600E protein, making it a valuable tool for cancer research aimed at understanding and addressing mutant BRAF-driven tumors. Its ability to modulate protein levels through targeted ubiquitination offers significant potential for therapeutic applications in oncology.

Cat. No.

A40728

CAS No.

2417296-82-1

PROTAC BRAF-V600E degrader-2

PROTAC BRAF-V600E Degrader-2 is a highly selective degrader targeting the BRAF-V600E mutant, with dissociation constants (Kd) of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. This compound effectively induces degradation of the BRAF-V600E kinase domain without impacting wild-type BRAF. Its potent biological activity makes it a valuable tool for research applications focused on melanoma cell growth inhibition and the study of BRAF-related signaling pathways.