PF-562271
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
- 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
- color
- Off-white to light yellow
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.
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