| 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. |
Selective |
B-Raf, IC50: 0.13 nM |
| 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. |
Selective |
B-Raf, Ki: 0.16 nM |
| 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. |
Selective |
B-Raf, IC50: 10 nM; B-Raf, Kd: 2.4 nM |
| 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. |
Selective |
B-Raf, IC50: 3 nM-60 nM |
| 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. |
Selective |
|
| 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. |
Pan |
|
| 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. |
Pan |
B-Raf (V600E), IC50: 0.7 nM; B-Raf, IC50: 5.2 nM |
| 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. |
Pan |
B-Raf (V600E), IC50: 0.7 nM; B-Raf, IC50: 5.2 nM |
| 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. |
Pan |
B-Raf(V600E), Ki: 1 nM |
| 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. |
Pan |
B-Raf, IC50: 1.5 nM; BRAF(V600E), IC50: 1 nM |
| 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. |
Pan |
BRAF(V600E), IC50: 3.8 nM; BRAF, IC50: 14 nM |
| 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. |
Pan |
BRAF(V600E), IC50: 5.8 nM; BRAF WT, IC50: 15 nM |
| 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. |
Pan |
BRAF WT, IC50: 41 nM; BRAF V600E, IC50: 7 nM |
| 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.
|
Pan |
BRAF V600E, IC50: 8.2 nM; BRAF, IC50: 19 nM |
| 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. |
Pan |
B-Raf, IC50: 8.3 nM |
| 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. |
Pan |
B-Raf (V600E), IC50: 13 nM; B-Raf, IC50: 160 nM |
| 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. |
Pan |
B-Raf (V600E), Kd: 14 nM; B-Raf, Kd: 36 nM |
| 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. |
Pan |
B-Raf, IC50: 28 nM; B-Raf (V600E), IC50: 19 nM |
| 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. |
Pan |
B-Raf (V600E), IC50: 19 nM; B-Raf, IC50: 28 nM |
| 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. |
Pan |
B-Raf, IC50: 22 nM |
| 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. |
Pan |
B-Raf, IC50: 22 nM; B-Raf (V599E), IC50: 38 nM |
| 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. |
Pan |
B-Raf, IC50: 22 nM; B-Raf (V599E), IC50: 38 nM |
| 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.
|
Pan |
BRAF(V600E), IC50: 23 nM; BRAF WT, IC50: 32 nM |
| 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. |
Pan |
B-Raf, IC50: 24 nM |
| 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. |
Pan |
B-Raf (V600E), IC50: 31 nM; B-Raf, IC50: 100 nM |
| 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. |
Pan |
B-Raf (V600E), IC50: 34 nM; B-Raf, IC50: 105 nM |
| 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. |
Pan |
WT BRAF, IC50: 79 nM; BRAF(V600E), IC50: 38 nM |
| S7743 |
CCT196969 |
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
Pan |
BRAF, IC50: 0.1 μM |
