Raf

Sigaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	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

Raf Inhibitors (20)
Raf Chemicals (1)
New Raf Products

Catalog No.	Information	Product Use Citations	Product Validations
S1267	Vemurafenib (PLX4032, RG7204) Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.	Nature, 2015, 10.1038/nature14336 Nature, 2014, 508(7494):118-22 Nature, 2012, 483(7387):100-3	The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).
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.	Hepatology, 2013, 59(4):1435-47 Blood, 2013, 122(9):1621-33 Blood, 2012, 120(19):4104-15	Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 μM), JNK inhibitor (16 μM), p38 inhibitor SB203580 (20 μM), and multikinase inhibitor sorafenib (10 μM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.
S1152	PLX-4720 PLX4720 is a potent and selective inhibitor of B-Raf^V600E 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.	Nat Biotechnol, 2013, 31(7):630-7 Nature, 2015, 517(7536):583-8 Nature, 2013, 498(7452):109-12	Combinatorial knockdown of NF1 and C-RAF abrogates NF1-mediated resistance to B-RAF inhibition at the level of ERK phosphorylation. A375 cells were infected with NF1 shRNA and treated with either DMSO or PLX4720 for 16 h. Cell lysates were analyzed for the indicated proteins.
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.	Science, 2016, 352(6282):189-96 J Clin Invest, 2014, 124(3):1406-17 J Clin Invest, 2014, 124(11):5074-84	A375P cells were treated with vehicle, the BRAF inhibitor GSK2118436, the MEK inhibitor GSK1120212, 10 uM HCQ, or the indicated combinations. Shown are 48-hour immunoblots directed against the indicated proteins.
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.	Cancer Discov, 2013, 3(3):350-62 J Natl Cancer Inst, 2012, 104(21):1673-9 P Natl Acad Sci USA, 2011, 108(15):6067-72	Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.
S7743^New	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.	Hepatology, 2012, 56(6):2363-74 Mol Cell Proteomics, 2012, 11(6):M112.017764 Pigment Cell Melanoma Res, 2014, 27(1):124-33	Raf265 inhibited the kinase activity of B-Raf but not of Raf-1 in Pkd2cKO cholangiocytes. Cells were treated for 30 min with different concentrations of Raf265. B-Raf and Raf-1 were immunoprecipated as described in the methods section and a kinase assay in vitro was performed using MEK as a substrate. The kinase activity of Raf was assessed by immunoblot analysis and quantified as optical density of pMEK with respect to untreated cells. In WT cholangiocytes (A) Raf265 inhibited both B-Raf and Raf-1 kinase activity. In Pkd2cKO cholangiocytes (B), Raf265 inhibited only B-Raf while a biphasic effect was found in Raf-1 with a significant increase at doses from 0.001 to 1 uM and a significant inhibition at 10 uM. Blots are representative of four different experiments. (p<0.05 vs controls; *p<0.001 vs controls).
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.	Cancer Discov, 2013, 3(3):350-62 Stem Cells, 2015, 10.1002/stem.1990 Oncotarget, 2014, 5(21):10732-44	A375 cells were infected with the indicated shRNAs/ORFs. In parallel to the above, cells were also treated with 0.2 uM AZ628 for 16 h, cell lysates were analyzed by Western blotting for the indicated proteins.
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.	J Pharmacol Sci, 2015, 129(1):65-71 Anticancer Res, 2014, 34(6):2913-8
S2220	SB590885 SB590885 is a potent B-Raf inhibitor with K_i 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.	Cell Death Dis, 2014, 5:e1278 Oncotarget, 2015, 6(17):15250-64 J Steroid Biochem Mol Biol, 2016, 10.1016/j.jsbmb.2016.09.009	Western blotting of the indicated proteins in WM266-4 cells treated for 48 h with 1 μM of BRAF (PLX4032 or SB590885) or MEK (AZD6244 or AS703026) inhibitors.
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.	Pharm Biol, 2016, 54(4):732-9	Effect of inhibitors on EAP’s proliferation activity in NIH3T3 cell by MTT assay. Data are presented as mean ± SD of three independent experiments. **p50.01 versus EAP.
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.	Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913 Hepatology, 2013, 59(4):1435-47 Blood, 2013, 122(9):1621-33	Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 μM), JNK inhibitor (16 μM), p38 inhibitor SB203580 (20 μM), and multikinase inhibitor sorafenib (10 μM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.
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.	Clin Cancer Res, 2015, 21(19):4420-30 Clin Cancer Res, 2014, 20(9):2410-23 Mol Cell Proteomics, 2012, 11(9):745-57	Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 °C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle-alone control, 27 °C represents temperature rescue of F508-CFTR at 27 °C, 37 °C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity.
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.	Oncotarget, 2016, 7(7):8172-83	Graph showing a concentration-dependent response of hypoxia-induced HIF-1α-NanoLuc activity to RAS-RAF-MEK-ERK pathway inhibitors: GDC-0994, PD-184352, selumetinib, TAK632, trametinib, and vemurafenib.
S8015	CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with K_d 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.	Cancer Lett, 2016, 370(2):332-44	(E) A375 and G361 cells were transfected with GFP-mRFP-LC3 for 24 h, then they were treated the same as in (D) for 4 and 24 h. Images were taken with a confocal microscope.
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.	Cell Rep, 2016, 10.1016/j.celrep.2016.05.064 Leukemia, 2017, 31(4):922-933	(a) INA-6, MM.1S, KMS11 or U266 cells were treated for 24 h either with 50 μm of the pan-Raf inhibitor MLN-2480, or 20 μm (INA-6 and MM.1S) or 25 μm (KMS11 or U266) of the pan-Raf inhibitor LY3009120 before western analyses of MEK1/2 and ERK1/2 activation with phosphorylation-specific antibodies.
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-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.	Nature, 2015, 10.1038/nature14336 Nature, 2014, 508(7494):118-22 Nature, 2012, 483(7387):100-3	The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).
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.	Hepatology, 2013, 59(4):1435-47 Blood, 2013, 122(9):1621-33 Blood, 2012, 120(19):4104-15	Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 μM), JNK inhibitor (16 μM), p38 inhibitor SB203580 (20 μM), and multikinase inhibitor sorafenib (10 μM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.
S1152	PLX-4720 PLX4720 is a potent and selective inhibitor of B-Raf^V600E 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.	Nat Biotechnol, 2013, 31(7):630-7 Nature, 2015, 517(7536):583-8 Nature, 2013, 498(7452):109-12	Combinatorial knockdown of NF1 and C-RAF abrogates NF1-mediated resistance to B-RAF inhibition at the level of ERK phosphorylation. A375 cells were infected with NF1 shRNA and treated with either DMSO or PLX4720 for 16 h. Cell lysates were analyzed for the indicated proteins.
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.	Science, 2016, 352(6282):189-96 J Clin Invest, 2014, 124(3):1406-17 J Clin Invest, 2014, 124(11):5074-84	A375P cells were treated with vehicle, the BRAF inhibitor GSK2118436, the MEK inhibitor GSK1120212, 10 uM HCQ, or the indicated combinations. Shown are 48-hour immunoblots directed against the indicated proteins.
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.	Cancer Discov, 2013, 3(3):350-62 J Natl Cancer Inst, 2012, 104(21):1673-9 P Natl Acad Sci USA, 2011, 108(15):6067-72	Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.
S7743^New	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.	Hepatology, 2012, 56(6):2363-74 Mol Cell Proteomics, 2012, 11(6):M112.017764 Pigment Cell Melanoma Res, 2014, 27(1):124-33	Raf265 inhibited the kinase activity of B-Raf but not of Raf-1 in Pkd2cKO cholangiocytes. Cells were treated for 30 min with different concentrations of Raf265. B-Raf and Raf-1 were immunoprecipated as described in the methods section and a kinase assay in vitro was performed using MEK as a substrate. The kinase activity of Raf was assessed by immunoblot analysis and quantified as optical density of pMEK with respect to untreated cells. In WT cholangiocytes (A) Raf265 inhibited both B-Raf and Raf-1 kinase activity. In Pkd2cKO cholangiocytes (B), Raf265 inhibited only B-Raf while a biphasic effect was found in Raf-1 with a significant increase at doses from 0.001 to 1 uM and a significant inhibition at 10 uM. Blots are representative of four different experiments. (p<0.05 vs controls; *p<0.001 vs controls).
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.	Cancer Discov, 2013, 3(3):350-62 Stem Cells, 2015, 10.1002/stem.1990 Oncotarget, 2014, 5(21):10732-44	A375 cells were infected with the indicated shRNAs/ORFs. In parallel to the above, cells were also treated with 0.2 uM AZ628 for 16 h, cell lysates were analyzed by Western blotting for the indicated proteins.
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.	J Pharmacol Sci, 2015, 129(1):65-71 Anticancer Res, 2014, 34(6):2913-8
S2220	SB590885 SB590885 is a potent B-Raf inhibitor with K_i 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.	Cell Death Dis, 2014, 5:e1278 Oncotarget, 2015, 6(17):15250-64 J Steroid Biochem Mol Biol, 2016, 10.1016/j.jsbmb.2016.09.009	Western blotting of the indicated proteins in WM266-4 cells treated for 48 h with 1 μM of BRAF (PLX4032 or SB590885) or MEK (AZD6244 or AS703026) inhibitors.
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.	Pharm Biol, 2016, 54(4):732-9	Effect of inhibitors on EAP’s proliferation activity in NIH3T3 cell by MTT assay. Data are presented as mean ± SD of three independent experiments. **p50.01 versus EAP.
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.	Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913 Hepatology, 2013, 59(4):1435-47 Blood, 2013, 122(9):1621-33	Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 μM), JNK inhibitor (16 μM), p38 inhibitor SB203580 (20 μM), and multikinase inhibitor sorafenib (10 μM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.
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.	Clin Cancer Res, 2015, 21(19):4420-30 Clin Cancer Res, 2014, 20(9):2410-23 Mol Cell Proteomics, 2012, 11(9):745-57	Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 °C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle-alone control, 27 °C represents temperature rescue of F508-CFTR at 27 °C, 37 °C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity.
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.	Oncotarget, 2016, 7(7):8172-83	Graph showing a concentration-dependent response of hypoxia-induced HIF-1α-NanoLuc activity to RAS-RAF-MEK-ERK pathway inhibitors: GDC-0994, PD-184352, selumetinib, TAK632, trametinib, and vemurafenib.
S8015	CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with K_d 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.	Cancer Lett, 2016, 370(2):332-44	(E) A375 and G361 cells were transfected with GFP-mRFP-LC3 for 24 h, then they were treated the same as in (D) for 4 and 24 h. Images were taken with a confocal microscope.
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.	Cell Rep, 2016, 10.1016/j.celrep.2016.05.064 Leukemia, 2017, 31(4):922-933	(a) INA-6, MM.1S, KMS11 or U266 cells were treated for 24 h either with 50 μm of the pan-Raf inhibitor MLN-2480, or 20 μm (INA-6 and MM.1S) or 25 μm (KMS11 or U266) of the pan-Raf inhibitor LY3009120 before western analyses of MEK1/2 and ERK1/2 activation with phosphorylation-specific antibodies.
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.

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S2200

Raf265 derivative

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

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Isoform-specific Inhibitors