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In A20 cells, PF-431396 blocks anti-Ig- and clustering LFA-1-induced tyrosine phosphorylation of Pyk2 and FAK, and further blocks B cell spreading. PF-431396 consistently inhibits the increase in protein tyrosine phosphorylation (PY) induced by the absence of added calcium and induced by W-7 in the presence of calcium.
| Molecular Weight | 506.5 |
| Formula | C22H21F3N6O3S |
| CAS Number | 717906-29-1 |
| Solubility (25°C) | 100 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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. |
| PF-00562271
PF-00562271 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. |
| Defactinib
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor, with potential antiangiogenic and antineoplastic activities. |
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