braf inhibitor

BRAF inhibitor is an inhibitor of B-Raf.

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

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

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.

B-Raf IN 14 is a BRAF inhibitor.

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].

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

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

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

Encorafenib (LGX818) is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.

RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.

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.

Binimetinib (ARRY-162) is a MEK1 2 inhibitor (IC50=12 nM) with selective and oral activity. Binimetinib has antitumor activity for the treatment of metastatic melanoma that cannot be resected or has a BRAF V600E or V600K mutation.

B-Raf IN 2, compound Ia, is a highly effective and specific inhibitor of BRAF. It exhibits significant potential for cancer research.

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

PLX8394 is an orally active inhibitor of serine threonine-protein kinase B-Raf (BRAF) protein. PLX8394 can selectively bind to and inhibit the activity of both wild-type and mutated forms of BRAF, then inhibit the proliferation of tumor cells which express mutated forms of BRAF. PLX8394 appears to be effective against tumors that express multiple mutated forms of the kinase and may be an effective therapeutic agent for tumors that are resistant to other BRAF inhibitor therapies that are specific for the BRAF V600E mutant.

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

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.

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.

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

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

Tinlorafenib (PF-07284890) (compound 10) is an orally active, central nervous system (CNS)-permeable BRAF kinase inhibitor targeting BRAFV600E (IC50: 4.25 nM) and V600K (IC50: 2.7 nM). Tinlorafenib is applicable for studying BRAF-associated malignant and benign tumors of the CNS and extracranial malignancies.

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.

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.

Uplarafenib (B-Raf IN 10) is a potent BRAF inhibitor with an IC50 of 50-100 nM. B-Raf IN 10 exhibits antitumor activity that may influence cell proliferation and differentiation, making it suitable for studying solid tumors.

VEGFR-2/BRAF-IN-1, a dual inhibitor of VEGFR-2 and BRAF kinases, demonstrates potent inhibitory activity with IC50 values of 0.049 µM for VEGFR-2, 0.063 µM for BRAF V600E, and 0.005 µM for BRAF WT. It effectively induces apoptosis and arrests the cell cycle primarily at the G1/S phase.

REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B

Everafenib is a potent BRAF inhibitor that crosses the blood-brain barrier and also inhibits the MAPK pathway. Everafenib inhibits the activity of a range of V600EBRAF melanoma cell lines (IC50: 2-10 nM) and is more effective than Dabrafenib and Vemurafenib. Everafenib was effective in extending the number of days of survival in a mouse model of intracranial metastatic melanoma.

Vem-L-Cy5 (compound 3), a Vemurafenib-based BRAF inhibitor conjugated with the near-infrared (NIR) fluorophore cyanine-5 (Cy5), selectively targets the BRAF V600E mutation and inhibits MEK phosphorylation. This compound demonstrates cell permeability and has been shown to inhibit the growth of various cancer cell types [1].

ARQ 736 is a potent and selective BRAF inhibitor. ARQ 736 is selectively potent in killing cancer cell lines harboring at least one mutated BRAF allele. BRAF mutations were detected in over 60% of melanomas and may account for a significant proportion of colon cancer patients whose tumors are resistant to anti-EGFR therapy. The B-Raf protein is a key signaling molecule in the mitogen activated protein kinase (MAPK) signaling pathway and has been implicated in the pathogenesis of a variety of cancers.

VEGFR-2/BRAF-IN-2, as a dual VEGFR-2 and BRAF kinase inhibitor, exhibits potent IC50 values of 0.111 µM, 0.089 µM, and 0.071 µM against VEGFR-2, BRAF V600E, and BRAF WT, respectively. This compound effectively induces apoptosis and predominantly arrests the cell cycle in the G1 phase.

SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA

RAS RAS-RAF-IN-1 is a potent inhibitor of RAS and RAS-RAF, exhibiting a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity and demonstrating antitumor activity[1].

EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb.

Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1 2 inhibitor used in treating proliferative diseases characterized by activating mutations in the MAPK pathway, particularly KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC), and KRAS-mutant ovarian cancer[1].

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.

PF-04880594 is a potent and selective RAF inhibitor targeting both wild-type and mutant BRAF and CRAF, exhibiting antitumor activity [1].

Lifirafenib (BGB-283) maleate, a novel inhibitor targeting both Raf Kinase and EGFR, exhibits potent activity with IC50 values of 23 nM and 29 nM against recombinant BRaf V600E and EGFR, respectively [1].

PLX7922, a RAF inhibitor, demonstrates binding affinity with BRAF V600E and exhibits inhibitory effects on pERK in BRAF V600E cell lines, while inducing pERK activation in mutant NRAS cell lines.

EGFR/BRAF-IN-1, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent inhibitor of EGFR/BRAF, inhibiting BRAFV600E (IC50:45 nM) and cancer cell proliferation (GI50=35 nM), with good antioxidant effect.

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.