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PF-00562271 (PF-562271) is a potent ATP-competitive FAK and proline-rich tyrosine kinase (Pyk2) inhibitor with potential antineoplastic and antiangiogenic activities. Focal adhesion kinase (FAK) transduces signaling from integrins and growth factors to modulate tumor cell invasion, proliferation and survival. Focal adhesion kinase (FAK) is a non-receptor protein tyrosine kinase located in the cytoplasm at focal adhesions – sites that link the extracellular matrix to the cytoplasmic cytoskeleton. Not only do FAKs therefore play a pivotal role in cell migration, but they also influence cell survival and are upregulated in a broad spectrum of epithelial cancers. PF-00562271 (PF-562271) may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by PF-00562271 (PF-562271) may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.
| Cell Experiment | |
|---|---|
| Cell lines | Squamous cell carcinoma (SCC) |
| Preparation method | Plating cells for 48 hours before addition of PF-562271. 3 days later, cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Washing the plates with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm.Using GraphPad Prism 4 software for curve fitting and carrying out generation of IC50 values from six replicates. |
| Concentrations | 0 to 1 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | PC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic female mice |
| Formulation | PF-562271 is dissolved in 5% Gelucire. |
| Dosages | ≤100 mg/kg |
| Administration | Administered via p.o. |
| Molecular Weight | 665.66 |
| Formula | C21H20F3N7O3S.C6H6O3S |
| CAS Number | 939791-38-5 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Brian Y Lee, et al. FAK signaling in human cancer as a target for therapeutics
| Related FAK Products |
|---|
| NVP-TAE226
Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM. |
| PF-562271
PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively. |
| PF-573228
PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
| Defactinib
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor, with potential antiangiogenic and antineoplastic activities. |
| PND-1186
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. |
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