braf inhibitor

BRAF inhibitor is an inhibitor of B-Raf.

B-Raf inhibitor 1 (B-Raf inhibitor 1) is a potent and selective B-Raf inhibitor.

Raf inhibitor 1 dihydrochloride (B-Raf inhibitor 1 dihydrochloride) is a potent and selective B-Raf inhibitor.

SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC50=4/1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.

Encorafenib (LGX818) is an oral, highly selective inhibitor of the BRAF V600E mutation with an IC50 of 0.3 nM, exhibiting antitumor activity. Encorafenib can be used for studying tumor signaling pathway regulation and mechanisms of drug resistance.

B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity, demonstrating an IC50 of 3.55 nM in the [BRAF V600E] enzyme assay.

Xl-281 (BMS-908662) is a BRAF inhibitor with anti-tumor activity for the study of colorectal cancer and melanoma.

B-Raf IN 15 is a BRAF inhibitor that inhibits BRAFWT and BRAFV600E and can be used in the study of melanoma and cancer, and can be optimized for use as a more effective BRA F inhibitor.

B-Raf IN 16, a BRAF inhibitor, belongs to cyclic iminopyrimidine derivatives and can be used for cancer or tumour research.

CCT241161 is an orally active pan-RAF inhibitor, with IC50 values of 3, 6, 10, 15, and 30 nM for LCK, CRAF, SRC, V600E-BRAF, and BRAF, respectively. It exhibits significant activity against BRAF and NRAS mutant melanomas and demonstrates anticancer cell proliferative effects [1].

INU-152 is a pan-RAF inhibitor. INU-152 has potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer. INU-152 inhibits all RAF isoforms and inhibits MAPK pathways in mutant BRAF cells. INU-152 exhibits minimal paradoxical pathway activa

SIJ1777 is a pyrimidopyrimidinone class type II pan-BRAF inhibitor, optimized as a derivative of GNF-7. It exerts anti-tumor effects by simultaneously inhibiting the phosphorylation and activation of the MAPK pathway (MEK/ERK) and the PI3K/AKT pathway. The core advantage of SIJ1777 is its ability to maintain double-digit nanomolar GI50 values against class II/III BRAF mutants (non-V600 mutants) and NRAS-mutant melanoma cells that are insensitive to current clinical drugs (such as vemurafenib, PLX8394), effectively inducing apoptosis and blocking tumor cell migration and anchorage-independent growth.

OPN-9652 is a potent and orally active covalent TEAD inhibitor, with a half-maximal inhibitory concentration (IC50) of 0.005 µM against TEAD in MSTO-211H cells, and it targets the central palmitate-binding pocket of TEAD. OPN-9652 can significantly reduce the activity of TEAD-dependent reporter genes and downregulate the expression levels of TEAD target genes (CTGF and CYR61). Notably, OPN-9652 can reverse the resistance of SOX10 knockout (SOX10 KO) resistant cells to the combination of BRAF inhibitor (BRAFi) and MAPK inhibitor (MAPKi), restoring their sensitivity to the drugs. In the xenograft mouse model of BRAF-mutant A375 cells, OPN-9652 can effectively delay the development of tumor drug resistance; specifically, this effect is manifested by a significant delay in the onset of tumor drug resistance after the combination of BRAFi and MEK inhibitor (MEKi) starting from the minimal residual disease (MRD) stage. At present, OPN-9652 can be used as a research tool for scientific research related to melanoma.

B-Raf IN 14 is a BRAF inhibitor.

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

B-Raf IN 1 is an inhibitor of B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM).

DS03090629, an orally active MEK inhibitor, functions by competitively inhibiting MEK activity in the presence of ATP. This compound demonstrates strong binding affinity to both MEK and phosphorylated MEK, with dissociation constants (Kd) of 0.11 and 0.15 nM, respectively. It has shown efficacy in suppressing the proliferation of melanoma cell lines that overexpress BRAF mutations, achieving IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 is thus considered promising for anti-melanoma therapies.

KRASG12C IN-14 (compound 15), a potent inhibitor specifically designed for the KRAS G12C mutation, exhibits impressive efficacy in impeding CYPA-dependent KRAS-BRAF interaction and ERK phosphorylation in NCI-H358 cells, both with an IC 50 of 0.002 μM.

MEK/RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK/RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

SJ-C1044 is an orally effective pan-RAF inhibitor demonstrating immunomodulatory and antitumor activities. It targets wild-type BRAF, wild-type CRAF, and BRAF(V600E) with IC50 values of 331, 257, and 187 nM, respectively. SJ-C1044 suppresses tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. Additionally, it shows inhibition of VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM respectively. The compound enhances the tumor immune microenvironment through inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is applicable for research in colorectal cancer.

JNK-IN-18 (compound 23b) is a potent inhibitor of JNK1, boasting an IC50 of 2 nM. It demonstrates superior efficacy when compared to its IC50 values of 125 nM for JNK2 and 98 nM for BRAF(V600E).

Claturafenib (PF-07799933) is a brain-permeable, selective, all-mutant BRAF inhibitor with broad inhibitory effects on pERK levels in HT29 cells.Claturafenib has shown antitumor activity in preclinical studies in both BRAF V600- and non-V600-mutant cancers and can be used in combination with MEK inhibitors.

BRAFV600E-IN-1 (compound 9S) is an inhibitor of BRAF. It exhibits significant apoptotic effects in cell lines expressing mutant KRAS and cancer cells harboring BRAFV600E.