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Raf Inhibitors | Chemicals (16)


Cat.No. Product Name Information Product Citations Customer Reviews
S1267 Vemurafenib (PLX4032, RG7204) Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.
  • Nature, 2012, 483(7387):100-3
  • Nature, 2014, 508(7494):118-22
  • Cell, 2012, 151(5):937-50
S1040 Sorafenib Tosylate Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
  • Hepatology, 2013, 59(4):1435-47
  • Blood, 2012, 120(19):4104-15
  • Blood, 2013, 122(9):1621-33
S1152 PLX-4720 PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
  • Nature, 2013, 498(7452):109-12
  • Nature, 2012, 483(7387):100-3
  • Nat Biotechnol, 2013, 31(7):630-7
S2807 Dabrafenib (GSK2118436) Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, 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
  • Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1392
S1104 GDC-0879 GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM 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
  • Proc Natl Acad Sci U S A, 2011, 108(15):6067-72
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.
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, respectively.
  • J Neurosci, 2013, 33(7):3079-93
  • Mol Oncol, 2014, 10.1016/j.molonc.2014.05.005
  • J Cell Sci, 2014, 127(Pt 7):1585-94
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, respectively, showing less or no inhibition against other tested kinases.
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. 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, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
  • Cancer Discov, 2013, 3(3):350-62
  • Cell Death Dis, 2014, 5:e1278
Cat.No. Product Name Information Product Citations Customer Reviews
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.
  • Anticancer Res, 2014, 34(6):2913-8
S2220 SB590885 SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
  • Cell Death Dis, 2014, 5:e1278
  • 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.
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, 2014, 20(9):2410-23
  • Mol Cell Proteomics, 2012, 11(9):745-57
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.
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