brafv600e

Agerafenib hydrochloride, a highly potent inhibitor of BRAFV600E (Kd: 14 nM), demonstrates significant efficacy.

CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.

BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3, and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM, and 0.009 μM, respectively. It also inhibits the phosphorylation of MEK1/2 and ERK1/2. Additionally, BRAFV600E/JNK-IN-1 suppresses tumor cell proliferation, NO release, and PGE2 production, exhibiting both antitumor and anti-inflammatory activities.

EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual inhibitor of EGFR and BRAFV600E, with IC50 values of 61 nM and 43 nM, respectively. It halts the cell cycle, induces apoptosis in both early and late stages, and inhibits cancer cell growth in vitro, showing broad-spectrum anticancer activity.

EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual inhibitor targeting both BRAFV600E and EGFR, with IC50 values of 0.048 μM and 0.037 μM, respectively. It exhibits potent anti-melanoma activity, showing IC50 values of 3.16 μM for MALME-3M cells and 2.50 μM for LOX-IMVI cells. The compound exerts its antitumor effects by inducing G1 phase arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 is useful for melanoma research, especially in studies focusing on the combined inhibition of the BRAFV600E mutation and EGFR signaling pathways.

EGFR/BRAFV600E-IN-1 (Compound 23) is a potent dual inhibitor of EGFR (IC50: 0.08 μM) and BRAFV600E (IC50: 0.15 μM), exhibiting anti-proliferative effects on A-549 (IC50: 1.2 μM), MCF-7 (IC50: 0.79 μM), Panc-1 (IC50: 1.3 μM), and HT-29 (IC50: 1.23 μM).

EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively. It induces apoptosis and exhibits promising antioxidant activity [1].

E07 Aptamer, targeting the human epidermal growth factor receptor (hEGFR), competes with epidermal growth factor (EGF) for binding to a unique epitope on EGFR. This aptamer not only binds to EGFR-expressing cells but also inhibits receptor autophosphorylation and thwarts tumor cell proliferation in three-dimensional matrices, positioning it as a useful tool for tumor disease research [1].

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.

RAF mutant-IN-1 is an inhibitor of RAF kinase(IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively).

HG6-64-1 is a potent and selective inhibitor of B-Raf, with an IC50 of 0.09 μM on B-raf V600E-transformed Ba/F3 cells.

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

BRAF V600E/CRAF-IN-1 is a potent inhibitor of BRAFV600E/CRAF. BRAF V600E/CRAF-IN-1 acts in the G0/G1 phase of HCT-116 colon cancer cells to arrest the cell cycle and cause apoptosis. BRAF V600E/CRAF-IN-1 shows potential for cancer disease research.

BRAF V600E/CRAF-IN-2 is a potent inhibitor of BRAFV600E/CRAF with IC50 values of 0.888 and 0.229 μM, respectively.BRAF V600E/CRAF-IN-2 induces cell cycle arrest at G0/G1 phase and apoptosis in HCT-116 colon cancer cells.BRAF V600E/CRAF-IN-2 has shown research potential for cancer disease. CRAF-IN-2 has shown potential for research into cancer disease.

PROTAC BRAF-V600E degrader-2 is a useful organic compound for research related to life sciences. The catalog number is T8744 and the CAS number is 2417296-82-1.

TBAP-001 is a RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay and an IC50 of 18 nM in Cell-Based Phosho-ERK Assay.

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.

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

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

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.

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.

Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRafV600E), 8.86 nM (ARaf), 5.78 nM (BRafWT), and 1.65 nM (CRaf). It exhibits antiproliferative activity against various cancer cell lines and can be utilized in cancer research.

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.