FAK (Focal Adhesion Kinase, or PTK2) is a protein tyrosine kinase that is not associated with receptors and is not located on membranes. It is activated at the sites of integrin clustering and cell-matrix adhesions by autophosphorylation (at Tyr397), Src, and other tyrosine kinases. By transferring signals governing cell migration, adhesion, and survival from the extracellular matrix to the cytoplasm, FAK mediates integrin-based cell signaling.
Many tumors, including those from the head and neck, colon, breast, prostate, liver, and thyroid, overexpress FAK. Additionally, in these tumors, FAK overexpression is strongly associated with an invasive phenotype. Glioblastomas and ovarian cancer cells are less likely to invade when dominant-negative FAK fragments are overexpressed and FAK signaling is inhibited. FAK is a crucial target for the creation of anti-metastatic and anti-neoplastic medications.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V0663 | Defactinib (VS6063, PF04554878) | 1073154-85-4 | Defactinib (formerly known as VS-6063, PF-04554878) is a selective, ATP-competitive and orally bioactive small molecule inhibitor of the FAK (focal adhesion kinase) with potential antitumor activity. |
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V0656 | PF-00562271 besylate | 939791-38-5 | PF-00562271 besylate (also called PF562271 or PF-562271 Besylate), the benzenesulfonate salt form of PF-00562271, is an ATP-competitive and orally bioavailable inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with potential antitumor activity. |
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V0661 | PF-431396 | 717906-29-1 | PF-431396 (PF431396) is a pyrimidine-based and selectivedual inhibitor of PYK2 and FAK (focal adhesion kinase and proline-rich tyrosine kinase 2) with potential anti-osteoporoticactivity. |
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V2696 | PF-562271 | 717907-75-0 | PF-562271 is a novel, potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with a IC50 of 1.5 and 14 nmol/L, respectively. |
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V0660 | PF-562271 HCl | 939791-41-0 | PF-562271 HCl is the hydrochloride salt of PF-562271 (PF562271 or PF 562271), which is a potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 (proline-rich tyrosine kinase) catalytic activity with potential anticancer activity. |
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V0658 | PF-573228 | 869288-64-2 | PF-573228 (PF573228) is a selective andATP-competitive FAK (focal adhesion kinase) inhibitorwith potential antitumor activity. |
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V0662 | PND-1186 (VS-4718; SR-2156) | 1061353-68-1 | PND-1186 (also known as SR2156, PND1186 or VS4718) is a novel, potent, reversible and selective FAK (focal adhesion kinase) inhibitor with potential anticancer activities. |
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V0659 | TAE226 (NVP-TAE226) | 761437-28-9 | TAE226 (also known as NVP-TAE226; TAE-226) is a novel, potent, selective and ATP competitive small molecule FAK(focal adhesion kinase) inhibitor with potential antineoplastic activity. |
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