ChemicalBook > CAS DataBase List > PF-562271

PF-562271

Product Name
PF-562271
CAS No.
939791-38-5
Chemical Name
PF-562271
Synonyms
PF-00562271, >=98%;PF-562271 (besylate);PF-00562271 Besylate;PF-562271 PhSO3H salt;PF-00562271 (PF-562271);PF-562271 benzenesulfonate;LKLWTLXTOVZFAE-UHFFFAOYSA-N;PF-562271 besylate PF562271;PF 562271 Benzenesulfonic acid;PF-562271 benzenesulfonate salt
CBNumber
CB22535568
Molecular Formula
C27H26F3N7O6S2
Formula Weight
665.66
MOL File
939791-38-5.mol
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PF-562271 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P330Rinse mouth.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0387
Product name
PF-562,271
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$166
Updated
2025/07/31
Sigma-Aldrich
Product number
PZ0387
Product name
PF-562,271
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$436
Updated
2025/07/31
Cayman Chemical
Product number
18499
Product name
PF-562271 (besylate)
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
18499
Product name
PF-562271 (besylate)
Purity
≥98%
Packaging
5mg
Price
$161
Updated
2024/03/01
Cayman Chemical
Product number
18499
Product name
PF-562271 (besylate)
Purity
≥98%
Packaging
10mg
Price
$266
Updated
2024/03/01
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PF-562271 Chemical Properties,Usage,Production

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

PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3[1]. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo[3].

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

Raw materials

Preparation Products

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939791-38-5, PF-562271Related Search:


  • 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
  • PF-00562271 benzenesulfonate salt
  • PF-00562271 benzesulfonate-data
  • LKLWTLXTOVZFAE-UHFFFAOYSA-N
  • N-methyl-N-(3-{[2-(2-oxo-2,3-dihydro-1H-indol-5-ylamino)-5-trifluoromethylpyrimidin-4-ylamino]methyl}pyridin-2-yl)methanesulfonamide monobesylate
  • PF562271 BESYLATE;PF 562271 BESYLATE
  • PF-00562271 Besylate
  • PF-562271 (benzesulfonate salt)
  • PF-562271 besylate PF562271
  • PF 562271 Benzenesulfonic acid
  • PF-562271 besylate, 10 mM in DMSO
  • 939791-38-5
  • C21H20F3N7O3SC6H6O3S
  • Inhibitors