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
-
Bioact Mater, 2022, 18:459-470
-
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
|
|
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
-
Am J Cancer Res, 2022, 12(4):1912-1918
|
|
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
-
EMBO Mol Med, 2022, 14(3):e15295
-
Cell Rep, 2022, 38(10):110490
|
|
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. |
-
Sci Signal, 2022, 15(728):eabj6915
-
Biology (Basel), 2022, 11(1)121
-
Immunity, 2021, S1074-7613(21)00403-9
|
|
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. |
-
Biochem J, 2022, 479(3):401-424
-
Elife, 2021, 10e73430
-
Front Cell Dev Biol, 2021, 9:785055
|
|
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
-
Cell Death Dis, 2022, 13(4):351
-
Drug Chem Toxicol, 2022, 1-10
|
|
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. |
-
Bioact Mater, 2022, 18:459-470
-
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
-
Cell Mol Life Sci, 2022, 79(5):228
|
|
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
- Bioact Mater, 2022, 18:459-470
- Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
|
|
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
- Am J Cancer Res, 2022, 12(4):1912-1918
|
|
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
- EMBO Mol Med, 2022, 14(3):e15295
- Cell Rep, 2022, 38(10):110490
|
|
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. |
- Sci Signal, 2022, 15(728):eabj6915
- Biology (Basel), 2022, 11(1)121
- Immunity, 2021, S1074-7613(21)00403-9
|
|
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. |
- Biochem J, 2022, 479(3):401-424
- Elife, 2021, 10e73430
- Front Cell Dev Biol, 2021, 9:785055
|
|
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
- Cell Death Dis, 2022, 13(4):351
- Drug Chem Toxicol, 2022, 1-10
|
|
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
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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
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S6538 |
B-Raf IN 1
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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. |
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S6660 |
B-Raf inhibitor 1 (Compound 13) dihydrochloride
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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
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S6680 |
L-779450
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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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S6905 |
MCP110
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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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S7108 |
Encorafenib (LGX818)
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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
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S7121 |
Tovorafenib (MLN2480)
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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
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S7170 |
RO5126766 (CH5126766)
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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.
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- EMBO Mol Med, 2021, e11814
- Cancer Sci, 2021, 112(10):4026-4036
- Nature, 2020, 588(7838):509-514
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S7291 |
TAK-632
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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
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S7397 |
Sorafenib (BAY 43-9006)
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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. |
- Bioact Mater, 2022, 18:459-470
- Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
- Cell Mol Life Sci, 2022, 79(5):228
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S7743 |
CCT196969
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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
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S7842 |
LY3009120
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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
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S7926 |
Lifirafenib (BGB-283)
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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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- Nat Commun, 2020, 11(1):3157
- Cell Rep, 2020, 31(11):107764
- Cell Rep, 2019, 29(3):573-588
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S7964 |
PLX7904
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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
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S7965 |
PLX8394
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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
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S8015 |
Agerafenib (RXDX-105)
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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
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S8189 |
BAW2881 (NVP-BAW2881)
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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
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S8690 |
RAF709
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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
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S8745 |
Naporafenib (LXH254)
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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
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S8755 |
AZ304
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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. |
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S8853 |
Belvarafenib (HM95573)
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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
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S9621 |
Donafenib (Sorafenib D3)
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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. |
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