MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1)
- Product Name
- MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1)
- CAS No.
- 939791-41-0
- Chemical Name
- MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1)
- Synonyms
- PF-562271 HCl ，S7357;PF-562271 hydrochloride;PF562271 HCL;PF 562271 HCL;PF562271 hydrochloride. PF271, PF-271, PF 271;N-methyl-N-(3-{[2-(2-oxo-2,3-dihydro-1H-indol-5-ylamino)-5-trifluoromethylpyrimidin-4-ylamino]methyl}pyridin-2-yl)methanesulfonamide hydrochloride;PF562271; PF562271; PF-562271; PF562,271; PF562,271; PF-562,271; PF-00562271; PF00562271; PF 00562271; PF562271 HYDROCHLORIDE. PF271, PF-271, PF 271;N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide:hydrochloride;MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1);Proline-rich tyrosine kinase 2,Ewing,inhibit,Antitumor,PF-562271,Focal adhesion kinase,Sarcoma,FAK,VS-6062(hydrochloride),PTK2 protein tyrosine kinase 2,Pyk2,PF562271 hydrochloride,PTK2,PF 562271,PF562271,Cancer,PF 562271 hydrochloride,Inhibitor,Breast
- CBNumber
- CB82667582
- Molecular Formula
- C21H21ClF3N7O3S
- Formula Weight
- 543.95
- MOL File
- 939791-41-0.mol
MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1) Property
- storage temp.
- Store at -20°C
- solubility
- ≥26.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
- form
- solid
N-Bromosuccinimide Price
- Product number
- A8345
- Product name
- PF-562271HCl
- Packaging
- 5mg
- Price
- $120
- Updated
- 2021/12/16
- Product number
- A8345
- Product name
- PF-562271HCl
- Packaging
- 10mg
- Price
- $190
- Updated
- 2021/12/16
MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1) Chemical Properties,Usage,Production
Uses
PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively[1].
Biological Activity
pf-562271 is a potent, atp-competitive and reversible inhibitor of both focal adhesion kinase (fak), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (pyk2), an fak homolog containing 48% amino acid identity, with half maximal inhibitory concentration (ic50) of 1.5 nmol/l and 14 nmol/l respectively. as a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, pf-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits fak phosphorylation in tumor-bearing mice with half maximal effective concentration (ec50) of 93 ng/ml.
in vivo
PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC50 of 93 ng/mL, total) after p.o. administration to tumor-bearing mice[1]. Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor[3].
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.
MethanesulfonaMide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)aMino]-5-(trifluoroMethyl)-4-pyriMidinyl]aMino]Methyl]-2-pyridinyl]-N-Methyl-, hydrochloride (1:1) Preparation Products And Raw materials
Raw materials
Preparation Products
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