PF-562271 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

A potent, ATP-competitive and reversible inhibitor of FAK and Pyk2 catalytic activity with IC50s of 1.5 nM and 14 nM, respectively.

Enzyminhibitor

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.

PF-562271 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

PF-562271 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32965	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	29810	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32161	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	22787	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
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	trendseenbio@gmail.com	China	11681	58

717907-75-0()Verwandte Suche:

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• N-Methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide PF-562271
• PF 562271 N-Methyl-N-[3-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
• PF-562271, >=98%
• N-Methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyrid
• N-METHYL-N-[3-[[[2-[(2-OXO-1,3-DIHYDROINDOL-5-YL)AMINO]-5-(TRIFLUOROMETHYL)PYRIMIDIN-4-YL]AMINO]METHYL]PYRIDIN-2-YL]METHANESULFONAMIDE
• N-Methyl-N-[3-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-trifluoromethylpyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
• PF-00562271
• PF 562271
• N-Methyl-N-(3-((2-(2-oxoindolin-5-ylaMino)-5-(trifluoroMethyl)pyriMidin-4-ylaMino)Methyl)pyridin-2-yl)MethanesulfonaMide
• PF-562271 free base
• PF562271/PF-562271
• N-Methyl-N-[3-[[[2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)aMino]-5-trifluoroMethylpyriMidin-4-yl]aMino]Methyl]pyridin-2-yl]MethanesulfonaMide (PF-562271)
• Methanesulfonamide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-
• N-[3-[[[2-[(2,3-Dihydro-2-oxo-1h-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-n-methyl-methanesulfonamide
• PF-562271 USP/EP/BP
• CS-2148
• CS-17
• 717907-75-0
• C21H20F3N7O3S
• Inhibitors
• PF562271