Src

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Src Inhibitors (11)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1021 Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
  • Cell Stem Cell, 2012, 10(2):210-7
  • Cancer Discov, 2011, 1(7):608-25
  • Sci Transl Med, 2015, 7(284):284ra57
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.
  • Nat Cell Biol, 2014, 16(5):401-14
  • Nat Cell Biol, 2013, 15(4):395-405
  • J Clin Invest, 2014, 124(12):5490-502
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.
  • Blood, 2011, 118(7):1885-98
  • Cancer Res, 2010, 70(19):7489-99
  • Mol Cell Biol, 2012, 32(2):320-32
S2700 KX2-391 KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
S7008 PP2 PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
  • Oncogene, 2015, 10.1038/onc.2015.12
S7774 SU6656 SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
S7782 Dasatinib Monohydrate Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
S7565 WH-4-023 WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50 of 2 nM and 6 nM, respectively.
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
S7060 PP1 PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
  • J Virol, 2011, 85(5):2296-304
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2391 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.
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All Src Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1021 Dasatinib <1 mg/mL 98 mg/mL <1 mg/mL
S1006 Saracatinib (AZD0530) <1 mg/mL 100 mg/mL 100 mg/mL
S1014 Bosutinib (SKI-606) <1 mg/mL 100 mg/mL 2 mg/mL
S2700 KX2-391 <1 mg/mL 86 mg/mL <1 mg/mL
S7008 PP2 <1 mg/mL 60 mg/mL 2 mg/mL
S7774 SU6656 <1 mg/mL 74 mg/mL <1 mg/mL
S7782 Dasatinib Monohydrate <1 mg/mL 21 mg/mL <1 mg/mL
S7565 WH-4-023 <1 mg/mL 12 mg/mL 6 mg/mL
S2202 NVP-BHG712 <1 mg/mL 101 mg/mL 3 mg/mL
S7060 PP1 <1 mg/mL 4 mg/mL <1 mg/mL
S2391 Quercetin <1 mg/mL 61 mg/mL 10 mg/mL
Tags: Src activation | Src kinase family | Src family kinases | Src activity | Src cancer | Src tyrosine kinase | Src pathway | Src phosphorylation | Src inhibition | Src kinase pathway | Src kinase assay | Src inhibitors cancer | Src inhibitor clinical trials | Src inhibitor review
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