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;N-Methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyrid;N-Methyl-N-(3-((2-(2-oxoindolin-5-ylaMino)-5-(trifluoroMethyl)pyriMidin-4-ylaMino)Methyl)pyridin-2-yl)MethanesulfonaMide
- CBNumber:
- CB72484683
- Molecular Formula:
- C21H20F3N7O3S
- Molecular Weight:
- 507.49
- MDL Number:
- MFCD16038299
- MOL File:
- 717907-75-0.mol
| 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 |
| FDA UNII | K5BX8ZA7UF |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P280-P305+P351+P338 |
PF-562271 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | P293920 | PF-562271 | 717907-75-0 | 2.5mg | $90 | 2021-12-16 | Buy |
| Usbiological | 215890 | PF-562271 | 717907-75-0 | 1mg | $339 | 2021-12-16 | Buy |
| Usbiological | 474161 | PF 562271 | 717907-75-0 | 100mg | $1848 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb180786 | PF-562271 >98% | 717907-75-0 | 1g | $2097.8 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb180786 | PF-562271 >98% | 717907-75-0 | 100mg | $615.4 | 2021-12-16 | Buy |
PF-562271 Chemical Properties,Uses,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
PF-56227 is a potent, ATP-competitive, reversible inhibitor of focal adhesion kinase (FAK). Potent FAK inhibitor.
Uses
A potent, ATP-competitive and reversible inhibitor of FAK and Pyk2 catalytic activity with IC50s of 1.5 nM and 14 nM, respectively.
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.
PF-562271 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49374 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29811 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32165 | 58 |
| Allfluoro pharmaceutical co. ltd. | 021-26137118 +8615821363818 | sales@allfluoro.com | China | 5790 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 22883 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
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