FAK

FAK製品

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  • FAK阻害剤 (17)
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S2890 PF-562271 PF-562271 (PF-00562271) 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.
Heliyon, 2024, 10(1):e23690
Nat Commun, 2023, 14(1):6270
Cell Death Dis, 2023, 14(2):135
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. PF-573228 induces apoptosis.
Bioact Mater, 2023, 20:598-609
Nat Commun, 2023, 14(1):6777
Cancers (Basel), 2023, 15(13)3379
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Clin Cancer Res, 2024, 30(1):187-197
Signal Transduct Target Ther, 2023, 8(1):11
Gut, 2023, gutjnl-2022-327927
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
J Exp Med, 2023, 220(9)e20230054
Adv Sci (Weinh), 2023, 10(10):e2205397
J Thromb Haemost, 2023, 21(8):2236-2247
S7653 VS-4718 (PND-1186) VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
Cell Death Dis, 2024, 15(2):108
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
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.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S2672 PF-562271 Besylate PF-562271 Besylate 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.
Elife, 2023, 12RP89141
bioRxiv, 2023, 2023.06.02.543509
Front Immunol, 2022, 13:837180
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. TAE226 (NVP-TAE226) induces apoptosis.
Theranostics, 2022, 12(3):1097-1116
Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119
Cancer Res Treat, 2022, 54(3):767-781
S8523 GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
Research (Wash D C), 2023, 6:0215
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
Nat Commun, 2023, 14(1):6270
Cell Rep, 2023, 42(5):112529
J Exp Clin Cancer Res, 2021, 40(1):364
S5321 Y15 Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
Cells, 2023, 12(15)1964
J Cell Sci, 2023, 136(15)jcs261001
Int J Biol Sci, 2022, 18(13):5019-5037
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
E0806 Narmafotinib Narmafotinib (AMP-945) is an inhibitor of focal adhesion kinase (FAK).
E1113 GSK215 GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader, which exerts FAK degradation in A549 non-small-cell lung cancer cells with DC50 of 1.3 nM by a strong time-dependence way and maximal degradation (Dmax) near the limit of the assay quantification (Dmax 99%).
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.
S2360 Solanesol (Nonaisoprenol) Solanesol (Nonaisoprenol, Betulanonaprenol) is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants.
S2890 PF-562271 PF-562271 (PF-00562271) 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.
Heliyon, 2024, 10(1):e23690
Nat Commun, 2023, 14(1):6270
Cell Death Dis, 2023, 14(2):135
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. PF-573228 induces apoptosis.
Bioact Mater, 2023, 20:598-609
Nat Commun, 2023, 14(1):6777
Cancers (Basel), 2023, 15(13)3379
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Clin Cancer Res, 2024, 30(1):187-197
Signal Transduct Target Ther, 2023, 8(1):11
Gut, 2023, gutjnl-2022-327927
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
J Exp Med, 2023, 220(9)e20230054
Adv Sci (Weinh), 2023, 10(10):e2205397
J Thromb Haemost, 2023, 21(8):2236-2247
S7653 VS-4718 (PND-1186) VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
Cell Death Dis, 2024, 15(2):108
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
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.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S2672 PF-562271 Besylate PF-562271 Besylate 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.
Elife, 2023, 12RP89141
bioRxiv, 2023, 2023.06.02.543509
Front Immunol, 2022, 13:837180
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. TAE226 (NVP-TAE226) induces apoptosis.
Theranostics, 2022, 12(3):1097-1116
Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119
Cancer Res Treat, 2022, 54(3):767-781
S8523 GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
Research (Wash D C), 2023, 6:0215
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
Nat Commun, 2023, 14(1):6270
Cell Rep, 2023, 42(5):112529
J Exp Clin Cancer Res, 2021, 40(1):364
S5321 Y15 Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
Cells, 2023, 12(15)1964
J Cell Sci, 2023, 136(15)jcs261001
Int J Biol Sci, 2022, 18(13):5019-5037
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
E0806 Narmafotinib Narmafotinib (AMP-945) is an inhibitor of focal adhesion kinase (FAK).
E1113 GSK215 GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader, which exerts FAK degradation in A549 non-small-cell lung cancer cells with DC50 of 1.3 nM by a strong time-dependence way and maximal degradation (Dmax) near the limit of the assay quantification (Dmax 99%).
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.
S2360 Solanesol (Nonaisoprenol) Solanesol (Nonaisoprenol, Betulanonaprenol) is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants.

FAK阻害剤の選択性比較

FAKシグナル伝達経路

FAKシグナル伝達経路
Tags: FAK activation | FAK signaling | FAK cancer | FAK phosphorylation | Focal Adhesion Kinase cancer | Focal Adhesion Kinase signaling | FAK inhibition | Focal Adhesion Kinase activation | Focal Adhesion Kinase phosphorylation | FAK assay | FAK inhibitor clinical trial | FAK cleavage | FAK inhibitor review