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Raf Inhibitors | Chemicals (19)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Nature, 2015, 10.1038/nature14336
  • Nature, 2014, 508(7494):118-22
  • Nature, 2012, 483(7387):100-3
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
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.
  • Nat Biotechnol, 2013, 31(7):630-7
  • Nature, 2015, 517(7536):583-8
  • Nature, 2013, 498(7452):109-12
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.
  • J Clin Invest, 2014, 124(3):1406-17
  • J Clin Invest, 2014, 124(11):5074-84
  • Cell Res, 2015, 10.1038/cr.2015.56
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
S7121 MLN2480 MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.
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.
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
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
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
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Cell Death Dis, 2014, 5:e1278
  • J Cell Mol Med, 2015, 19(9):2244-52
  • Invest New Drugs, 2014, 32(4):626-35
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.
  • Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913
  • Hepatology, 2013, 59(4):1435-47
  • Blood, 2013, 122(9):1621-33
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
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.
S2200 Raf265 derivative Raf265 derivative, however, the effects of this derivative are not known.
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.
  • Cancer Lett, 2016, 370(2):332-44
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
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All Raf Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
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
S7121 MLN2480 <1 mg/mL 100 mg/mL 100 mg/mL
S7170 RO5126766 (CH5126766) <1 mg/mL 94 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
S7842 LY3009120 <1 mg/mL 3 mg/mL <1 mg/mL
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
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