PF-562271

PF-562271 속성

PF-562271 C화학적 특성, 용도, 생산

용도

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

효소 저해제

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 준비 용품 및 원자재

원자재

준비 용품

PF-562271 공급 업체

공급자	전화	이메일	국가	제품 수	이점
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	47465	58
career henan chemical co	+86-0371-86658258 15093356674;	factory@coreychem.com	China	29826	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Allfluoro pharmaceutical co. ltd.	021-26137118 +8615821363818	sales@allfluoro.com	China	5791	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29322	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58

PF-562271 관련 검색: