| Identification | Back Directory | [Name]
PF-562271 | [CAS]
939791-38-5 | [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-00562271 benzesulfonate-data
PF-562271 benzenesulfonate salt
PF-00562271 benzenesulfonate salt
PF562271 BESYLATE;PF 562271 BESYLATE
N-methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridin-2-yl)methanesulfonamide benzenesulfonate
N-methyl-N-(3-{[2-(2-oxo-2,3-dihydro-1H-indol-5-ylamino)-5-trifluoromethylpyrimidin-4-ylamino]methyl}pyridin-2-yl)methanesulfonamide monobesylate
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 | [Molecular Formula]
C27H26F3N7O6S2 | [MDL Number]
MFCD14105612 | [MOL File]
939791-38-5.mol | [Molecular Weight]
665.664 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,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 |
| Hazard Information | Back Directory | [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.1 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.2 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.2,3 | [Uses]
A potent, ATP-competitive and reversible inhibitor of FAK and Pyk2 catalytic activity with IC50s of 1.5 nM and 14 nM, respectively. | [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 | [storage]
Store at -20°C | [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. |
|
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
|