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FAK

FAK Products

All (22)
FAK Inhibitors (21)
FAK Activator (1)
New FAK Products

Catalog No.	Product Name	Information	Product Use Citations
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 Nat Commun, 2023, 14(1):6270
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.	Adv Mater, 2024, e2314358. Nat Commun, 2024, 15(1):2612 Theranostics, 2024, 14(7):3014-3028
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 Cell Death Dis, 2024, 15(9):678 Cell Death Dis, 2024, 15(5):370
S8032	PRT062607 (P505-15) HCl	PRT062607 (P505-15, BIIB057, PRT-2607) HCl 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.	Sci Rep, 2024, 14(1):7739 J Exp Med, 2023, 220(9)e20230054 J Exp Med, 2023, 220(9)e20230054
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.	Nat Commun, 2024, 15(1):3741 J Clin Invest, 2024, 134(19)e176828 Dev Cell, 2024, S1534-5807(24)00238-7
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.	Nat Cardiovasc Res, 2023, 2(6):550-571 Front Immunol, 2022, 13:837180 Cancers (Basel), 2022, 14(6)1537
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 Elife, 2023, 12RP89141 bioRxiv, 2023, 2023.06.02.543509
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.	Acta Neuropathol Commun, 2024, 12(1):40 Gut, 2023, gutjnl-2022-327927 Gut, 2023, 1–2
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 Nat Commun, 2023, 14(1):6270 Cell Rep, 2023, 42(5):112529
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 J Cell Sci, 2023, 136(15)jcs261001
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.
E1508^New	APG-2449	APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models.
E1961^New	NVL-655	NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively.
E1114^New	Ifebemtinib	Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo.
E1783^New	Conteltinib(CT-707)	Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay.
E0806	Narmafotinib	Narmafotinib (AMP-945) is an inhibitor of focal adhesion kinase (FAK).
E3677	Semen Ziziphi Spinosae Extract	Semen Ziziphi Spinosae Extract is extracted from the seeds of Semen Ziziphi Spinosae, which can attenuate blood-brain barrier dysfunction induced by lipopolysaccharide by targeting the FAK-DOCK180-Rac1-WAVE2-Arp3 signaling pathway.
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 Nat Commun, 2023, 14(1):6270
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.	Adv Mater, 2024, e2314358. Nat Commun, 2024, 15(1):2612 Theranostics, 2024, 14(7):3014-3028
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 Cell Death Dis, 2024, 15(9):678 Cell Death Dis, 2024, 15(5):370
S8032	PRT062607 (P505-15) HCl	PRT062607 (P505-15, BIIB057, PRT-2607) HCl 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.	Sci Rep, 2024, 14(1):7739 J Exp Med, 2023, 220(9)e20230054 J Exp Med, 2023, 220(9)e20230054
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.	Nat Commun, 2024, 15(1):3741 J Clin Invest, 2024, 134(19)e176828 Dev Cell, 2024, S1534-5807(24)00238-7
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.	Nat Cardiovasc Res, 2023, 2(6):550-571 Front Immunol, 2022, 13:837180 Cancers (Basel), 2022, 14(6)1537
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 Elife, 2023, 12RP89141 bioRxiv, 2023, 2023.06.02.543509
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.	Acta Neuropathol Commun, 2024, 12(1):40 Gut, 2023, gutjnl-2022-327927 Gut, 2023, 1–2
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 Nat Commun, 2023, 14(1):6270 Cell Rep, 2023, 42(5):112529
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 J Cell Sci, 2023, 136(15)jcs261001
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.
E1508^New	APG-2449	APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models.
E1961^New	NVL-655	NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively.
E1114^New	Ifebemtinib	Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo.
E1783^New	Conteltinib(CT-707)	Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay.
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.
E3677	Semen Ziziphi Spinosae Extract	Semen Ziziphi Spinosae Extract is extracted from the seeds of Semen Ziziphi Spinosae, which can attenuate blood-brain barrier dysfunction induced by lipopolysaccharide by targeting the FAK-DOCK180-Rac1-WAVE2-Arp3 signaling pathway.
E1508^New	APG-2449	APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models.
E1961^New	NVL-655	NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively.
E1114^New	Ifebemtinib	Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo.
E1783^New	Conteltinib(CT-707)	Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay.

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