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

InChIKey

LKLWTLXTOVZFAE-UHFFFAOYSA-N

SMILES

S(C1C=CC=CC=1)(O)(=O)=O.O=C1CC2=CC(NC3=NC=C(C(F)(F)F)C(NCC4C=CC=NC=4N(C)S(=O)(=O)C)=N3)=CC=C2N1

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).

in vivo

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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