FAK

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FAK Inhibitors (9)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2672 PF-00562271 PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
  • Mol Ther, 2012, 20(5):972-83
S2890 PF-562271 PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
  • J Biol Chem, 2015, 290(14):8677-92
  • Cancer Sci, 2013, 104(12):1618-25
  • PLoS One, 2014, 9(2):e88587
S2013 PF-573228 PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β.
  • J Biol Chem, 2015, 10.1074/jbc.M114.624247
  • PLoS One, 2014, 9(2):e88587
S2820 TAE226 (NVP-TAE226) TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.
  • Cell Death Dis, 2014, 5:e1134
  • J Biol Chem, 2015, 290(14):8677-92
S2725 PF-03814735 PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
  • Cancer Res, 2014, 74(20):5878-90
S7653 PND-1186 (VS-4718) PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.
S7654 Defactinib (VS-6063, PF-04554878) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
S7357 PF-562271 HCl PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
  • Cancer Sci, 2013, 104(12):1618-25
  • PLoS One, 2014, 9(2):e88587
  • Environ Toxicol Pharm, 2014, 39(1):114-124

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S2672 PF-00562271 <1 mg/mL 14 mg/mL <1 mg/mL
S2890 PF-562271 <1 mg/mL 100 mg/mL <1 mg/mL
S2013 PF-573228 <1 mg/mL 26 mg/mL <1 mg/mL
S2820 TAE226 (NVP-TAE226) <1 mg/mL 94 mg/mL <1 mg/mL
S2725 PF-03814735 <1 mg/mL 0.4 mg/mL <1 mg/mL
S7653 PND-1186 (VS-4718) <1 mg/mL 24 mg/mL <1 mg/mL
S7654 Defactinib (VS-6063, PF-04554878) <1 mg/mL 5 mg/mL <1 mg/mL
S7644 PF-431396 <1 mg/mL 100 mg/mL <1 mg/mL
S7357 PF-562271 HCl <1 mg/mL 100 mg/mL <1 mg/mL
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