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| | PF-562271 Basic information |
| Product Name: | PF-562271 | | Synonyms: | PF-562271 PhSO3H salt;PF-562271 benzenesulfonate salt;PF-00562271 (PF-562271);N-[3-[[[2-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-methanesulfonamide benzenesulfonate;PF-562271 (besylate);N-methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridin-2-yl)methanesulfonamide benzenesulfonate;PF-00562271, >=98%;PF-562271 benzenesulfonate | | CAS: | 939791-38-5 | | MF: | C27H26F3N7O6S2 | | MW: | 665.66 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 939791-38-5.mol |  |
| | PF-562271 Chemical Properties |
| storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | insoluble in EtOH; insoluble in H2O; ≥11.1 mg/mL in DMSO with gentle warming | | form | solid |
| | PF-562271 Usage And Synthesis |
| Description | Focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) are non-receptor tyrosine kinases that constitute the FAK subfamily and play a vital role in many oncogenic pathways. PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases. PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models. | | Uses | A potent, ATP-competitive and reversible inhibitor of FAK and Pyk2 catalytic activity with IC50s of 1.5 nM and 14 nM, respectively. | | Uses | PF 562271 Besylate is the besylate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of focal adhesion kinase (FAK). | | target | FAK | | references | [1]stokes jb, adair sj, slack-davis jk, walters dm, tilghman rw, hershey ed, lowrey b, thomas ks, bouton ah, hwang rf, stelow eb, parsons jt, bauer tw. inhibition of focal adhesion kinase by pf-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. mol cancer ther. 2011 nov;10(11):2135-45. doi: 10.1158/1535-7163.mct-11-0261. epub 2011 sep 8.
[2]roberts wg, ung e, whalen p, cooper b, hulford c, autry c, richter d, emerson e, lin j, kath j, coleman k, yao l, martinez-alsina l, lorenzen m, berliner m, luzzio m, patel n, schmitt e, lagreca s, jani j, wessel m, marr e, griffor m, vajdos f. antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, pf-562,271. cancer res. 2008 mar 15;68(6):1935-44. doi: 10.1158/0008-5472.can-07-5155. |
| | PF-562271 Preparation Products And Raw materials |
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