Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1267 Vemurafenib (PLX4032, RG7204) <1 mg/mL 97 mg/mL <1 mg/mL
S1040 Sorafenib Tosylate 0.01 mg/mL 127 mg/mL <1 mg/mL
S1152 PLX-4720 <1 mg/mL 83 mg/mL <1 mg/mL
S2807 Dabrafenib (GSK2118436) <1 mg/mL 30 mg/mL <1 mg/mL
S1104 GDC-0879 <1 mg/mL 66 mg/mL 5 mg/mL
S7965 PLX8394 <1 mg/mL 100 mg/mL <1 mg/mL
S8745 LXH254 <1 mg/mL 100 mg/mL 34 mg/mL
S5069 Dabrafenib Mesylate <1 mg/mL 100 mg/mL 5 mg/mL
S5077 Regorafenib Monohydrate -1 mg/mL 100 mg/mL -1 mg/mL
S8690 RAF709 <1 mg/mL 100 mg/mL 100 mg/mL
S2161 RAF265 (CHIR-265) <1 mg/mL 100 mg/mL 33 mg/mL
S2746 AZ 628 <1 mg/mL 90 mg/mL <1 mg/mL
S2202 NVP-BHG712 <1 mg/mL 101 mg/mL 3 mg/mL
S2220 SB590885 <1 mg/mL 5 mg/mL <1 mg/mL
S2720 ZM 336372 <1 mg/mL 78 mg/mL 2 mg/mL
S7397 Sorafenib <1 mg/mL 63 mg/mL <1 mg/mL
S2872 GW5074 <1 mg/mL 104 mg/mL <1 mg/mL
S7291 TAK-632 <1 mg/mL 100 mg/mL 2 mg/mL
S8015 CEP-32496(RXDX-105) <1 mg/mL 9 mg/mL <1 mg/mL
S7108 Encorafenib (LGX818) <1 mg/mL 100 mg/mL 100 mg/mL
S8189 BAW2881 (NVP-BAW2881) <1 mg/mL 84 mg/mL 20 mg/mL
S7743 CCT196969 <1 mg/mL 100 mg/mL <1 mg/mL
S7926 Lifirafenib (BGB-283) <1 mg/mL 95 mg/mL 95 mg/mL
S7964 PLX7904 <1 mg/mL 100 mg/mL <1 mg/mL
S7842 LY3009120 <1 mg/mL 3 mg/mL <1 mg/mL
S7170 RO5126766 (CH5126766) <1 mg/mL 94 mg/mL <1 mg/mL
S7121 MLN2480 <1 mg/mL 100 mg/mL 100 mg/mL
S2200 Raf265 derivative <1 mg/mL 101 mg/mL 101 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

Vemurafenib (PLX4032, RG7204)

Vemurafenib (PLX4032, RG7204) 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.


Sorafenib Tosylate

Sorafenib Tosylate is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.



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.


Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436) 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.



GDC-0879 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.



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.



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.


Dabrafenib Mesylate

Dabrafenib Mesylate 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.


Regorafenib Monohydrate

Regorafenib 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, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.



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.


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. Phase 2.


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.



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.



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.


ZM 336372

ZM 336372 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.



Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.



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.



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.



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, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.


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.


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 at 45-72 nM concentrations.



CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.


Lifirafenib (BGB-283)

Lifirafenib (BGB-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.



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.



LY03009120 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. Phase 1.


RO5126766 (CH5126766)

RO5126766 (CH5126766) 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.



MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.


Raf265 derivative

Raf265 derivative, however, the effects of this derivative are not known.

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