Raf

Sigaling 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
S7743 CCT196969 <1 mg/mL 100 mg/mL <1 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
S2200 Raf265 derivative <1 mg/mL 101 mg/mL 101 mg/mL
S8015 CEP-32496 <1 mg/mL 9 mg/mL <1 mg/mL
S7108 Encorafenib (LGX818) <1 mg/mL 100 mg/mL 100 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

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1267

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.

S1040

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.

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.

S2807

Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM in cell-free assays, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.

S1104

GDC-0879

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.

S7743New

CCT196969

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

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. Phase 2.

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.

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.

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.

S2720

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.

S7397

Sorafenib

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.

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.

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.

S8015

CEP-32496

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.

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.

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.

S7842

LY3009120

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.

S7170

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.

S7121

MLN2480

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

S2200

Raf265 derivative

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

Catalog No. Information Product Use Citations Product Validations
S1267

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.

S1040

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.

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.

S2807

Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM in cell-free assays, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.

S1104

GDC-0879

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.

S7743New

CCT196969

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

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. Phase 2.

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.

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.

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.

S2720

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.

S7397

Sorafenib

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.

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.

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.

S8015

CEP-32496

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.

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.

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.

S7842

LY3009120

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.

S7170

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.

S7121

MLN2480

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

Catalog No. Information Product Use Citations Product Validations
S2200

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