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SynKinase
PF-562271
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | PF562271 |
| Product Type | Chemical |
| Properties | |
| Formula | C21H20F3N7O3S |
| MW | 507.5 |
| CAS | 717907-75-0 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO or ethanol. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: FGFR | Kinase Group: RTK | Substrate: Tyrosine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | MZDKLVOWGIOKTN-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
PF-562,271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 catalytic activity with a IC(50) of 1.5 and 14nM, respectively. In addition, PF-562,271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5nM. PF-562,271 was evaluated against multiple kinases and displays >100x selectivity against a long list of nontarget kinases. In tests, PF-562,271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion with a calculated EC50 of 93ng/mL using injections.
Product References
- Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271: W.G. Roberts, et al.; Cancer Res. 68, 1935 (2008)
- Selectivity data: assessment, predictions, concordance, and implications. C. Gao, et al.; J. Med. Chem. 56, 6991 (2013)
- Integrating chemical and mechanical signals through dynamic coupling between cellular protrusions and pulsed ERK activation: J.M. Yang, et al.; Nat. Comm. 9, 4673 (2018)
- Src stimulates Abl-dependent phosphorylation of the guanine exchange factor Net1A to promote its cytosolic localization and cell motility: A. Sprenger, et al.; J. Biol. Chem. 104887 in press (2023)
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