Raf

Isoform-selective Products

Signaling Pathway

Raf Signaling Pathway

Raf Products

  • All (43)
  • Raf Inhibitors (43)
  • New Raf Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Biochem Pharmacol, 2024, 219:115952
Nat Cancer, 2023, 4(2):240-256
Nat Commun, 2023, 14(1):3251
S7397 Sorafenib Sorafenib 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.
Genomics, 2024, 116(1):110764
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S2807 Dabrafenib Dabrafenib is a mutant BRAFV600E 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.
Acta Neuropathol, 2024, 147(1):44
Front Immunol, 2024, 15:1334769
Drug Resist Updat, 2023, 71:100993
S1040 Sorafenib tosylate Sorafenib 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.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S1178 Regorafenib 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.
Nat Med, 2024, 10.1038/s41591-024-02824-y
NPJ Precis Oncol, 2024, 8(1):52
Signal Transduct Target Ther, 2023, 8(1):65
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.
Biosens Bioelectron, 2024, 10.1016/j.bios.2023.115819
Nat Commun, 2023, 14(1):1399
Nat Commun, 2023, 14(1):1399
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.
Aging Cell, 2024, e14093.
Cell Rep, 2023, 42(6):112547
Int J Mol Sci, 2023, 10.3390/ijms242216538
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.
Cells, 2023, 12(4)664
Nat Genet, 2022, 54(7):976-984
Nat Commun, 2022, 13(1):1100
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.
Drug Resist Updat, 2023, 71:100993
Exp Cell Res, 2023, 430(1):113722
Sci Adv, 2023, 9(28):eadf4766
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.
J Clin Med, 2023, 12(23)7267
J Hematol Oncol, 2022, 15(1):109
Life (Basel), 2022, 12(8)1258
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.
PLoS One, 2024, 19(1):e0295629
Nat Commun, 2022, 13(1):3706
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
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.
Sci Adv, 2023, 9(35):eade7486
Cancer Cell, 2022, S1535-6108(22)00312-9
Cancers (Basel), 2022, 14(21)5215
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.
Nat Commun, 2024, 15(1):668
PLoS One, 2024, 19(1):e0295629
Cell Stem Cell, 2023, 30(9):1235-1245.e6
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.
Int J Mol Sci, 2023, 24(7)6228
Sci Adv, 2023, 9(35):eade7486
Cell Syst, 2022, 13(11):885-894.e4
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
iScience, 2022, 25(10):105182
Cancers (Basel), 2022, 14(6)1575
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
Int J Mol Sci, 2021, 22(24)13175
Antibiotics (Basel), 2021, 10(10)1223
S7108 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.
Oncologist, 2024, 29(1):15-24
Nat Cancer, 2023, 4(2):240-256
Mol Cancer Ther, 2023, 22(2):227-239
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.
Cancers (Basel), 2023, 15(18)4477
Cancers (Basel), 2023, 15(18)4477
J Clin Med, 2023, 12(23)7267
S7170 Avutometinib Avutometinib(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.
Nature, 2022, 604(7905):354-361
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
Cell Mol Life Sci, 2022, 80(1):12
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, 2022, 41(11):111827
Oncogene, 2022, 10.1038/s41388-022-02519-z
Cell Rep, 2021, 35(1):108940
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.
Nat Commun, 2022, 13(1):4109
J Invest Dermatol, 2022, S0022-202X(22)00096-3
Mol Cancer Ther, 2020, 25;molcanther.1021.2019
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.
Cells, 2023, 12(4)664
ChemMedChem, 2023, e202300322.
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
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
Exp Gerontol, 2019, 126:110691
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, 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
Cancer Immunol Res, 2019,
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.
Sci Adv, 2023, 9(35):eade7486
J Clin Invest, 2021, e147849
J Clin Invest, 2021, e147849
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.
Sci Adv, 2023, 9(35):eade7486
Mol Cancer Ther, 2022, MCT-22-0004
Nat Commun, 2020, 11(1):3157
S7121 Tovorafenib (MLN2480) Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Sci Adv, 2023, 9(35):eade7486
Int J Hematol, 2021, 10.1007/s12185-021-03244-1
Cell Rep, 2019, 29(3):573-588
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.
Sci Adv, 2023, 9(35):eade7486
SLAS Discov, 2022, S2472-5552(22)12517-7
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
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.
Biomedicines, 2023, 11(4)1013
Osteoarthritis Cartilage, 2022, 30-11:1443-1454
Eur J Med Chem, 2017, 140:510-527
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
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
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Nat Commun, 2022, 13(1):7113
Cell Rep, 2019, 29(3):573-588
E1748New 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.
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.
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.
E1079 GNE-9815 GNE-9815 is a highly selective, pan-Raf inhibitor with good oral bioavailability. GNE-9815 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.
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.
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.
E1649New Exarafenib Exarafenib(KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases.
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.
Biochem Pharmacol, 2024, 219:115952
Nat Cancer, 2023, 4(2):240-256
Nat Commun, 2023, 14(1):3251
S7397 Sorafenib Sorafenib 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.
Genomics, 2024, 116(1):110764
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S2807 Dabrafenib Dabrafenib is a mutant BRAFV600E 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.
Acta Neuropathol, 2024, 147(1):44
Front Immunol, 2024, 15:1334769
Drug Resist Updat, 2023, 71:100993
S1040 Sorafenib tosylate Sorafenib 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.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S1178 Regorafenib 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.
Nat Med, 2024, 10.1038/s41591-024-02824-y
NPJ Precis Oncol, 2024, 8(1):52
Signal Transduct Target Ther, 2023, 8(1):65
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.
Biosens Bioelectron, 2024, 10.1016/j.bios.2023.115819
Nat Commun, 2023, 14(1):1399
Nat Commun, 2023, 14(1):1399
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.
Aging Cell, 2024, e14093.
Cell Rep, 2023, 42(6):112547
Int J Mol Sci, 2023, 10.3390/ijms242216538
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.
Cells, 2023, 12(4)664
Nat Genet, 2022, 54(7):976-984
Nat Commun, 2022, 13(1):1100
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.
Drug Resist Updat, 2023, 71:100993
Exp Cell Res, 2023, 430(1):113722
Sci Adv, 2023, 9(28):eadf4766
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.
J Clin Med, 2023, 12(23)7267
J Hematol Oncol, 2022, 15(1):109
Life (Basel), 2022, 12(8)1258
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.
PLoS One, 2024, 19(1):e0295629
Nat Commun, 2022, 13(1):3706
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
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.
Sci Adv, 2023, 9(35):eade7486
Cancer Cell, 2022, S1535-6108(22)00312-9
Cancers (Basel), 2022, 14(21)5215
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.
Nat Commun, 2024, 15(1):668
PLoS One, 2024, 19(1):e0295629
Cell Stem Cell, 2023, 30(9):1235-1245.e6
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.
Int J Mol Sci, 2023, 24(7)6228
Sci Adv, 2023, 9(35):eade7486
Cell Syst, 2022, 13(11):885-894.e4
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
iScience, 2022, 25(10):105182
Cancers (Basel), 2022, 14(6)1575
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
Int J Mol Sci, 2021, 22(24)13175
Antibiotics (Basel), 2021, 10(10)1223
S7108 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.
Oncologist, 2024, 29(1):15-24
Nat Cancer, 2023, 4(2):240-256
Mol Cancer Ther, 2023, 22(2):227-239
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.
Cancers (Basel), 2023, 15(18)4477
Cancers (Basel), 2023, 15(18)4477
J Clin Med, 2023, 12(23)7267
S7170 Avutometinib Avutometinib(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.
Nature, 2022, 604(7905):354-361
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
Cell Mol Life Sci, 2022, 80(1):12
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, 2022, 41(11):111827
Oncogene, 2022, 10.1038/s41388-022-02519-z
Cell Rep, 2021, 35(1):108940
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.
Nat Commun, 2022, 13(1):4109
J Invest Dermatol, 2022, S0022-202X(22)00096-3
Mol Cancer Ther, 2020, 25;molcanther.1021.2019
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.
Cells, 2023, 12(4)664
ChemMedChem, 2023, e202300322.
Proc Natl Acad Sci U S A, 2022, 119(5)e2113491119
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
Exp Gerontol, 2019, 126:110691
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, 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
Cancer Immunol Res, 2019,
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.
Sci Adv, 2023, 9(35):eade7486
J Clin Invest, 2021, e147849
J Clin Invest, 2021, e147849
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.
Sci Adv, 2023, 9(35):eade7486
Mol Cancer Ther, 2022, MCT-22-0004
Nat Commun, 2020, 11(1):3157
S7121 Tovorafenib (MLN2480) Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Sci Adv, 2023, 9(35):eade7486
Int J Hematol, 2021, 10.1007/s12185-021-03244-1
Cell Rep, 2019, 29(3):573-588
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.
Sci Adv, 2023, 9(35):eade7486
SLAS Discov, 2022, S2472-5552(22)12517-7
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
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.
Biomedicines, 2023, 11(4)1013
Osteoarthritis Cartilage, 2022, 30-11:1443-1454
Eur J Med Chem, 2017, 140:510-527
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
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
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Nat Commun, 2022, 13(1):7113
Cell Rep, 2019, 29(3):573-588
E1748New 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.
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.
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.
E1079 GNE-9815 GNE-9815 is a highly selective, pan-Raf inhibitor with good oral bioavailability. GNE-9815 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.
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.
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.
E1649New Exarafenib Exarafenib(KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases.
E1748New 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.
E1649New Exarafenib Exarafenib(KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases.

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