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FAK
FAK製品
- All (21)
- FAK阻害剤 (21)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|---|
| 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. |
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| 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. |
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| S7654 | Defactinib (VS-6063) | Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. | ||
| S7644 | PF-431396 | PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively. | ||
| 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. | ||
| 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. | ||
| E1508New | 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. | ||
| E1961New | 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. | ||
| E1114New | 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. | ||
| E1783New | 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. | ||
| 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. |
|
|
| 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. |
|
|
| S7654 | Defactinib (VS-6063) | Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| S7644 | PF-431396 | PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively. | ||
| 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. | ||
| 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. | ||
| E1508New | 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. | ||
| E1961New | 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. | ||
| E1114New | 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. | ||
| E1783New | 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. | ||
| E1508New | 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. | ||
| E1961New | 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. | ||
| E1114New | 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. | ||
| E1783New | 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. |
FAK阻害剤の選択性比較
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
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間