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Raf Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S2746 | AZ 628 | AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 induces apoptosis. |
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| S2220 | SB590885 | SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases. |
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| S7108 | LGX818 (Encorafenib) | Encorafenib is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3. |
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| S7291 | TAK-632 | TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases. |
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| S2872 | GW5074 | GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. This compound inhibits LK-induced apoptosis. |
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| S2161 | RAF265 (CHIR-265) | RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. This compound induces cell cycle arrest and apoptosis. Phase 2. |
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| S7965 | PLX8394 (Plixorafenib, FORE8394) | Plixorafenib (PLX8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity. |
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| S7964 | PLX7904 | PLX7904, 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. |
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| S2720 | ZM 336372 | ZM 336372 (Zinc00581684) is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc. |
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| S8745 | Naporafenib (LXH254) | Naporafenib (LXH254) is a type II ATP-competitive inhibitor that, at picomolar concentrations, inhibits both B- and CRAF kinase activities with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. |
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| S7121 | Tovorafenib (MLN2480) | Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials. |
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| S8015 | Agerafenib (CEP-32496) | Agerafenib (CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, respectively. It also shows potent activity against Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, but has insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. This compound is currently in Phase 1/2 clinical trials. |
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| S7926 | Lifirafenib (BGB-283) | Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays, with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. |
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| S8690 | RAF709 | RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM. |
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| S8853 | Belvarafenib | Belvarafenib is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively. |
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| S6660 | B-Raf inhibitor 1 (Compound 13) dihydrochloride | B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively. |
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| S7743 | CCT196969 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
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| S6680 | L-779450 | L-779450 is a highly potent low nanomolar inhibitor of B-raf with IC50 of 10 nM and Kd of 2.4 nM. |
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| E1748 | HG6-64-1 | HG6-64-1 (HMSL 10017-101-1) is a highly potent and selective inhibitor of B-Raf with an IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells. | ||
| E1682 | Tinlorafenib | Tinlorafenib (PF-07284890, ARRY-461) is a potent, brain-penetrant inhibitor of BRAF targeting V600E/V600K mutations with IC50 values of 4.25 nM and 2.7 nM, respectively. It also effectively inhibits ERK phosphorylation and represents a new class of selective BRAF inhibitors for brain tumors. | ||
| E2505 | TBAP-001 | TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-Raf kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay. | ||
| E8290New | Flezurafenib | Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity. | ||
| E1079 | GNE-9815 | GNE-9815 is a highly selective, pan-Raf inhibitor with good oral bioavailability. This compound exhibits Ki values of 0.062 and 0.19 nM for c-Raf and b-Raf, respectively. | ||
| S6538 | B-Raf IN 1 | B-Raf IN 1 is an inhibitor of Raf wih IC50 values of 24 nM and 25 nM for B-Raf and C-Raf respectively. It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα. | ||
| E2651 | Raf inhibitor 1 | Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively. | ||
| S9621 | Donafenib (Sorafenib D3) | Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. | ||
| E4681 | Claturafenib (PF-07799933) | Claturafenib (PF-07799933) is a brain-penetrant, selective, pan-mutant inhibitor of BRAF. It exhibits broad inhibition of pERK levels in HT29 cells with an IC50 value of 1.6 nM. This compound displays antitumor activity against BRAFV600- and non-V600-mutant cancers preclinically and in treatment-refractory patients. | ||
| E1965 | NST-628 | NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF. | ||
| E4599 | BGB-3245(Brimarafenib) | BGB-3245 (Brimarafenib) is an inhibitor of Raf kinase. This compound displays potent effects against different RAF isoforms, including BRAF Class I/II/III mutations, BRAF fusions, and heterodimerization with CRAF in preclinical models. It also exhibits antineoplastic effects. | ||
| E0934 | Raf inhibitor 2 | Raf inhibitor 2 is a potent Raf kinase inhibitor with an IC50 of <1.0 μM. | ||
| S8755 | AZ304 | AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site of wild type and V600E mutant BRAF with IC50 values of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R at sub 100 nM potencies. | ||
| S1178 | Regorafenib (BAY 73-4506) | Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
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| S1574 | Doramapimod (BIRB 796) | Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays. It binds p38α with Kd of 0.1 nM in THP-1 cells, showing 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, and insignificant inhibition of ERK-1, SYK, IKK2. |
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| S5077 | Regorafenib (BAY-734506) Monohydrate | Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) 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 (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
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| S4947 | Regorafenib Hydrochloride | Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
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| S2202 | NVP-BHG712 | NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; this compound also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. |
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| S8189 | BAW2881 (NVP-BAW2881) | BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. |
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| S6905 | MCP110 | MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. |
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