Raf

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Raf Signaling Pathways

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Catalog No. Product Name Information Product Use Citations Product Validations
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cancer Cell, 2022, S1535-6108(21)00662-0
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cancer Metab, 2022, 10(1):4
S1104 GDC-0879 GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
Cancer Lett, 2021, S0304-3835(21)00309-8
Cancers (Basel), 2021, 13(6)1205
Cell Syst, 2020, 10(3):240-253
S1152 PLX-4720 PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Blood Cancer J, 2022, 12(3):39
Oncogene, 2022, 10.1038/s41388-021-01920-4
Cancers (Basel), 2022, 14(6)1575
S1178 Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cell Rep, 2022, 38(10):110490
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Nat Commun, 2022, 13(1):1588
Cell Rep, 2022, 38(10):110490
Oncogene, 2022, 10.1038/s41388-021-01920-4
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, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
Biology (Basel), 2022, 11(1)121
Immunity, 2021, S1074-7613(21)00403-9
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
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. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.
Cancers (Basel), 2022, 14(6)1575
Drug Chem Toxicol, 2022, 1-10
J Clin Invest, 2021, e147849
S2202 NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; 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.
Cell Rep, 2021, 35(1):108940
Mol Ther Nucleic Acids, 2021, 25:328-341
Cancer Lett, 2020, 475:53-64
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.
Elife, 2021, 10e73430
Front Cell Dev Biol, 2021, 9:785055
Nat Commun, 2020, 11(1):5463
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.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
Cell Metab, 2020, 5;31(5):892-908 e11
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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.
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
Drug Chem Toxicol, 2022, 1-10
Cell Rep, 2021, 35(11):109233
S2807 Dabrafenib (GSK2118436) Dabrafenib (GSK2118436, GSK2118436A) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Cell Biol, 2022, 10.1038/s41556-022-00854-7
Nat Commun, 2022, 13(1):1381
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. GW5074 inhibits LK-induced apoptosis.
Cell Res, 2021, 10.1038/s41422-021-00532-7
Antibiotics (Basel), 2021, 10(10)1223
J Neurosci, 2020, 40(34):6522-6535
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.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Front Oncol, 2021, 11:796839
S5069 Dabrafenib Mesylate Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.
Nat Commun, 2022, 13(1):1381
Nat Commun, 2022, 13(1):1100
Drug Chem Toxicol, 2022, 1-10
S5077 Regorafenib (BAY-734506) Monohydrate Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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.
Pharmazie, 2022, 77(2):54-58
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
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.
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.
Eur J Med Chem, 2017, 140:510-527
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.
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.
S7108 Encorafenib (LGX818) Encorafenib (LGX818) 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.
Proc Natl Acad Sci U S A, 2022, 119(12):e2113535119
Drug Chem Toxicol, 2022, 1-10
Cell Rep, 2021, 35(8):109157
S7121 Tovorafenib (MLN2480) Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Int J Hematol, 2021, 10.1007/s12185-021-03244-1
Cell Rep, 2019, 29(3):573-588
Sci Rep, 2019, 9(1):636
S7170 RO5126766 (CH5126766) RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304) 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.
EMBO Mol Med, 2021, e11814
Cancer Sci, 2021, 112(10):4026-4036
Nature, 2020, 588(7838):509-514
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.
Cell Rep, 2021, 35(8):109157
Nat Commun, 2020, 11(1):4370
Nat Med, 2019, 25(2):284-291
S7397 Sorafenib (BAY 43-9006) Sorafenib (BAY 43-9006, NSC-724772) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cell Mol Life Sci, 2022, 79(5):228
Int J Mol Sci, 2022, 23(8)4277
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Cell Rep, 2019, 29(3):573-588
S7842 LY3009120 LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Nat Commun, 2022, 13(1):898
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
Nat Cell Biol, 2021, 23(4):377-390
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.
Nat Commun, 2020, 11(1):3157
Cell Rep, 2020, 31(11):107764
Cell Rep, 2019, 29(3):573-588
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.
J Invest Dermatol, 2022, S0022-202X(22)00096-3
Mol Cancer Ther, 2020, 25;molcanther.1021.2019
J Biol Chem, 2020, 295(8):2407-2420
S7965 PLX8394 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.
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
J Invest Dermatol, 2022, S0022-202X(22)00096-3
Sci Adv, 2021, 7(24)eabg0390
S8015 Agerafenib (RXDX-105) Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Mol Pharmacol, 2021, 99(6):435-447
Dis Model Mech, 2020, dmm.047779
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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.
JCI Insight, 2021, 143285
J Cell Biochem, 2019, 120(4):5583-5596
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.
Clin Cancer Res, 2020, 20 pii: clincanres
Cancer Res, 2020, canres.0448.2020
J Neurosci, 2020, 40(34):6522-6535
S8745 Naporafenib (LXH254) Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
J Clin Invest, 2021, e147849
J Clin Invest, 2021, e147849
Oncol Lett, 2021, 22(5):745
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.
S8853 Belvarafenib (HM95573) Belvarafenib (GDC5573, HM95573, RG6185) 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.
SLAS Discov, 2022, S2472-5552(22)12517-7
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
Cancer Biol Med, 2021, j.issn.2095-3941.2021.0137
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.
A5043 Raf1 Rabbit Recombinant mAb

Raf1 Antibody detects endogenous levels of total Raf1.

A5124 MEKK2 Rabbit Recombinant mAb MEKK2 Rabbit Recombinant mAb detects endogenous level of total MEKK2.
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cancer Cell, 2022, S1535-6108(21)00662-0
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cancer Metab, 2022, 10(1):4
S1104 GDC-0879 GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
Cancer Lett, 2021, S0304-3835(21)00309-8
Cancers (Basel), 2021, 13(6)1205
Cell Syst, 2020, 10(3):240-253
S1152 PLX-4720 PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Blood Cancer J, 2022, 12(3):39
Oncogene, 2022, 10.1038/s41388-021-01920-4
Cancers (Basel), 2022, 14(6)1575
S1178 Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cell Rep, 2022, 38(10):110490
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Nat Commun, 2022, 13(1):1588
Cell Rep, 2022, 38(10):110490
Oncogene, 2022, 10.1038/s41388-021-01920-4
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, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
Biology (Basel), 2022, 11(1)121
Immunity, 2021, S1074-7613(21)00403-9
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
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. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.
Cancers (Basel), 2022, 14(6)1575
Drug Chem Toxicol, 2022, 1-10
J Clin Invest, 2021, e147849
S2202 NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; 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.
Cell Rep, 2021, 35(1):108940
Mol Ther Nucleic Acids, 2021, 25:328-341
Cancer Lett, 2020, 475:53-64
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.
Elife, 2021, 10e73430
Front Cell Dev Biol, 2021, 9:785055
Nat Commun, 2020, 11(1):5463
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.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
Cell Metab, 2020, 5;31(5):892-908 e11
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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.
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
Drug Chem Toxicol, 2022, 1-10
Cell Rep, 2021, 35(11):109233
S2807 Dabrafenib (GSK2118436) Dabrafenib (GSK2118436, GSK2118436A) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Cell Biol, 2022, 10.1038/s41556-022-00854-7
Nat Commun, 2022, 13(1):1381
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. GW5074 inhibits LK-induced apoptosis.
Cell Res, 2021, 10.1038/s41422-021-00532-7
Antibiotics (Basel), 2021, 10(10)1223
J Neurosci, 2020, 40(34):6522-6535
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.
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
Front Oncol, 2021, 11:796839
S5069 Dabrafenib Mesylate Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.
Nat Commun, 2022, 13(1):1381
Nat Commun, 2022, 13(1):1100
Drug Chem Toxicol, 2022, 1-10
S5077 Regorafenib (BAY-734506) Monohydrate Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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.
Pharmazie, 2022, 77(2):54-58
ACS Appl Mater Interfaces, 2021, 13(41):48478-48491
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00223-X
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.
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.
Eur J Med Chem, 2017, 140:510-527
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.
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.
S7108 Encorafenib (LGX818) Encorafenib (LGX818) 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.
Proc Natl Acad Sci U S A, 2022, 119(12):e2113535119
Drug Chem Toxicol, 2022, 1-10
Cell Rep, 2021, 35(8):109157
S7121 Tovorafenib (MLN2480) Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Int J Hematol, 2021, 10.1007/s12185-021-03244-1
Cell Rep, 2019, 29(3):573-588
Sci Rep, 2019, 9(1):636
S7170 RO5126766 (CH5126766) RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304) 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.
EMBO Mol Med, 2021, e11814
Cancer Sci, 2021, 112(10):4026-4036
Nature, 2020, 588(7838):509-514
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.
Cell Rep, 2021, 35(8):109157
Nat Commun, 2020, 11(1):4370
Nat Med, 2019, 25(2):284-291
S7397 Sorafenib (BAY 43-9006) Sorafenib (BAY 43-9006, NSC-724772) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cell Mol Life Sci, 2022, 79(5):228
Int J Mol Sci, 2022, 23(8)4277
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Cell Rep, 2019, 29(3):573-588
S7842 LY3009120 LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Nat Commun, 2022, 13(1):898
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
Nat Cell Biol, 2021, 23(4):377-390
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.
Nat Commun, 2020, 11(1):3157
Cell Rep, 2020, 31(11):107764
Cell Rep, 2019, 29(3):573-588
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.
J Invest Dermatol, 2022, S0022-202X(22)00096-3
Mol Cancer Ther, 2020, 25;molcanther.1021.2019
J Biol Chem, 2020, 295(8):2407-2420
S7965 PLX8394 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.
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
J Invest Dermatol, 2022, S0022-202X(22)00096-3
Sci Adv, 2021, 7(24)eabg0390
S8015 Agerafenib (RXDX-105) Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
Mol Pharmacol, 2021, 99(6):435-447
Dis Model Mech, 2020, dmm.047779
Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
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.
JCI Insight, 2021, 143285
J Cell Biochem, 2019, 120(4):5583-5596
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.
Clin Cancer Res, 2020, 20 pii: clincanres
Cancer Res, 2020, canres.0448.2020
J Neurosci, 2020, 40(34):6522-6535
S8745 Naporafenib (LXH254) Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
J Clin Invest, 2021, e147849
J Clin Invest, 2021, e147849
Oncol Lett, 2021, 22(5):745
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.
S8853 Belvarafenib (HM95573) Belvarafenib (GDC5573, HM95573, RG6185) 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.
SLAS Discov, 2022, S2472-5552(22)12517-7
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
Cancer Biol Med, 2021, j.issn.2095-3941.2021.0137
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.
A5043 Raf1 Rabbit Recombinant mAb

Raf1 Antibody detects endogenous levels of total Raf1.

A5124 MEKK2 Rabbit Recombinant mAb MEKK2 Rabbit Recombinant mAb detects endogenous level of total MEKK2.
Tags: B-Raf inhibition | Raf inhibition | B-Raf mutation | B-Raf cancer | Raf tumor | Raf pathway | Raf inhibitor drugs | Raf activation | Raf targets | Raf activity | Raf phosphorylation | B-Raf assay | Raf kinase assay | B-Raf inhibitor clinical trial | B-Raf inhibitor drug | Raf inhibitor review