Raf

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Raf Inhibitors | Chemicals (17)

water-soluble

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
  • Cell, 2012, 151(5):937-50
  • Nat Med, 2012, 18(8):1239-47
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, 10.1002/hep.26790
  • Int J Cancer, 2012, 132(3):738-43
  • Blood, 2012, 120(19):4104-15
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. Phase 3.
  • J Clin Invest, 2014, 124(3):1406-17
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
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
  • Pigment Cell Melanoma Res, 2013, 27(1):124-33
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.
S7001 PF-04880594 PF-04880594 is a RAF inhibitor for BRAF/BRAFV599E and c-RAF with IC50 of 0.19 nM/0.13 nM and 0.39 nM, >100-fold selectivity over CSNK1, JNK2/3 and p38.
S7121 MLN2480 MLN-2480 (BIIB-024) is a pan-Raf inhibitor.
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.
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.
  • Apoptosis, 2013, 10.1007/s10495-013-0955-y
  • PLoS One, 2014, 9(2):e88587
Cat.No. Product Name Information Product Citations Customer Reviews
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
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
  • Proc Natl Acad Sci U S A, 2011, 108(15):6067-72
  • Cell Death Differ, 2012, 19(12):2029-39
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.
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.
  • Mol Cell Proteomics, 2012, 11(9):745-57
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.
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.
S2200 Raf265 derivative Raf265 derivative, however, the effects of this derivative are not known.
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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