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PF-562271

HY-10459

(PF562271; PF 562271)

PF-562271

PF-562271 Chemical Structure

PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $134 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
50 mg $450 Backordered
100 mg Get quote
200 mg Get quote
For PF-562271, please see related products:  PF-562271 besylate ,
Size Price Stock Quantity
10 mM * 1 mL in DMSO €131 In-stock
5 mg €118 In-stock
10 mg €186 In-stock
50 mg €441 Backordered
100 mg Get quote
200 mg Get quote
For PF-562271, please see related products:  PF-562271 besylate ,

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Product name: PF-562271
Cat. No.: HY-10459

PF-562271 Data Sheet

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    Purity: 99.58%

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Biological Activity of PF-562271

PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
IC50 value: 1.5 nM(FAK); 14 nM(Pyk2) [1]
Target: 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 [1]. 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 [2]. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels [3].
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 [1]. 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 [3].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 507.49 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C21H20F3N7O3S
CAS No 717907-75-0
Solvent & Solubility

DMSO 21 mg/ml

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.9705 mL 9.8524 mL 19.7048 mL
5 mM 0.3941 mL 1.9705 mL 3.9410 mL
10 mM 0.1970 mL 0.9852 mL 1.9705 mL

References on PF-562271

Other Forms

Inhibitor Kit

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