PF-562271
Description In vitro In vivo- Product Name
- PF-562271
- CAS No.
- 717907-75-0
- Chemical Name
- PF-562271
- Synonyms
- CS-17;CS-2148;PF 562271;PF-00562271;PF-562271, >=98%;PF562271/PF-562271;PF-562271 free base;PF-562271 USP/EP/BP;PF-562271, 10 mM in DMSO;N-Methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyrid
- CBNumber
- CB72484683
- Molecular Formula
- C21H20F3N7O3S
- Formula Weight
- 507.49
- MOL File
- 717907-75-0.mol
PF-562271 Property
- Melting point:
- >204°C (dec.)
- Density
- 1.540
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- White powder.
- pka
- 13.66±0.20(Predicted)
- color
- White to Off-White
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- P293920
- Product name
- PF-562271
- Packaging
- 2.5mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- 215890
- Product name
- PF-562271
- Packaging
- 1mg
- Price
- $339
- Updated
- 2021/12/16
- Product number
- 474161
- Product name
- PF 562271
- Packaging
- 100mg
- Price
- $1848
- Updated
- 2021/12/16
- Product number
- orb180786
- Product name
- PF-562271
- Purity
- >98%
- Packaging
- 1g
- Price
- $2097.8
- Updated
- 2021/12/16
- Product number
- orb180786
- Product name
- PF-562271
- Purity
- >98%
- Packaging
- 100mg
- Price
- $615.4
- Updated
- 2021/12/16
PF-562271 Chemical Properties,Usage,Production
Description
PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
In vitro
PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels.
In vivo
PF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose-and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia.
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-56227 is a potent, ATP-competitive, reversible inhibitor of focal adhesion kinase (FAK). Potent FAK inhibitor.
Definition
ChEBI: N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]methanesulfonamide is a member of indoles.
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.
Enzyme inhibitor
This potent, yet reversible ATP-competitive protein kinase inhibitor (FWfreebase = 507.49 g/mol; CAS 717907-75-0; FWHCl-Salt = 543.95 g/mol; FW = 665.66 g/mol (benzenesulfonate salt); CAS 939791-38-5), also named, N- [3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4- pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide, targets Focal Adhesion Kinase, or FAK, (IC50 = 1.5 nM), with about 10x greater potency than for Pyk2 (IC50 = 14 nM) and >100x more than for other protein kinases. PF-562271 binds within the ATP-binding cleft of FAK, where it forms two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the protein kinase’s hinge region. Mode of Inhibitory Action: Many cancer cells grow in an anchorage-independent manner, and the nonreceptor tyrosine kinase FAK is thought to contribute to this phenotype by localizing in focal adhesion plaques and has playing roles as a scaffolding and signaling component. Integrin signals within the tumor microenvironment also affect cancer cell survival and invasion during tumor progression, and FAK is activated by b-integrins in both normal and transformed cells. PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC50 = 93 ng/mL) after p.o. administration to tumor-bearing mice. PF-562271 also has potent effects on metastatic prostate cancer growth in vivo. Oral administration of PF-562271 at a dose of 5 mg/kg suppressed the growth and local spread of intratibial tumors and restored tumor-induced bone loss. The unique ability of PF-562271 to both curb tumor growth and safely increase bone formation may be an effective therapy for many cancer patients with bone metastases and cancer-associated osteoporosis.
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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View Lastest Price from PF-562271 manufacturers
- Product
- PF-562271 717907-75-0
- Price
- US $1.00/g
- Min. Order
- 100g
- Purity
- 98%min
- Supply Ability
- G/KG/T
- Release date
- 2019-12-20