b-raf (v600e)

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.

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.

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

PLX-4720 is a potent and selective B-Raf (V600E) inhibitor designed to block the ATP-binding site of oncogenic B-Raf with IC50 of 13 nM.

B-Raf IN 11 is a novel selective inhibitor. The DFG-in conformation of the B-Raf kinase V600E mutant is superior to the DFG-out conformation in colorectal cancer.

Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively.

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.

Plixorafenib (PLX8394) is an orally active inhibitor of the serine/threonine protein kinase B-Raf (BRAF) protein.Plixorafenib can selectively bind to and inhibit the activity of wild-type and mutant forms of BRAF, inhibiting the proliferation of tumor cells expressing mutant forms of BRAF.

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, effectively inhibiting BRAF (WT), BRAF (V600E), and wild-type CRAF [IC50s: 79/38/68 nM].

AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.

LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 values of 44 nM for A-raf, 31-47 nM for B-Raf, and 42 nM for C-Raf in A375 cells. Phase 1.

PLX7904 (PB04), also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.

RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.

BI-882370 is a specific RAF kinase inhibitor. BI-882370 inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases (IC50s: 0.4, 0.8 and 0.6 nM). BI-882370 also inhibits SRC family kinases.

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

EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual inhibitor of EGFR and BRAFV600E, with IC50 values of 0.12 μM and 0.05 μM, respectively. It exhibits antiproliferative activity against HT-29, MCF-7, A549, and Panc-1 cells, with IC50 values of 8, 4, 6, and 7 μM. EGFR/BRAFV600E-IN-6 activates caspase-3/8/9, upregulates Bax expression, and downregulates Bcl-2 levels, inducing apoptosis and exhibiting antioxidant properties. It is applicable in cancer research, such as studies on colon cancer.

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.

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-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.

BRAFV600E-IN-2 (compound 10) is a BRAFV600E inhibitor with an IC50 of less than 10 nM, demonstrating antitumor activity.

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).

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].