PF-562271 HCl

Catalog No.S7357

PF-562271 HCl Chemical Structure

Molecular Weight(MW): 543.95

PF-562271 HCl is the hydrochloride salt of PF-562271, which 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. Phase 1.

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Cited by 7 Publications

4 Customer Reviews

  • VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p < 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N > 4, ±SEM, *p < 0.05 vs respective control (D and E).

    Environ Toxicol Pharmacol 2014 39(1), 114-124. PF-562271 HCl purchased from Selleck.

    OVISE cells were incubated for 24 hr at the indicated concentrations of the FAK inhibitors. Immunoblots were performed to assess inhibition of auto-phosphorylation by the FAK inhibitors.

    PLoS One 2014 9(2), e88587. PF-562271 HCl purchased from Selleck.

  • NO production was increased in the netrin-1-over-expressing and recombinant netrin-1-treated MiaPaCa II cells. FAK inhibitor PF-562271 blocks the netrin-1-induced NO production. (*P < 0.05).

    Oncotarget, 2016, 7(17):24719-33.. PF-562271 HCl purchased from Selleck.

    Rat caudal arterial smooth muscle strips were pre-incubated for 30 min with PF-431396, PF-573228, PF-562271, NVP-TAE226, or sc-203950 (2 or 10 μm) or vehicle and then stimulated with K+ in the continued presence of inhibitor. A, force was recorded continuously, and values at 10 min after K+ addition are expressed relative to control K+-induced contractions. Values represent the mean ± S.E. (n = 6). *, p < 0.001, **, p < 0.002, significantly different from the control K+-induced sustained contractile response. B, tissues were quick-frozen 10 min after the addition of K+ for analysis of Pyk2 autophosphorylation by Western blotting with anti-pTyr-402-Pyk2 (pY402-Pyk2) and FAK autophosphorylation with anti-pTyr-397-FAK (pY397-FAK). Actin was used as the loading control, and anti-Pyk2 and anti-FAK were used to verify the total levels of the two proteins.

    J Biol Chem, 2015, 290(14):8677-92.. PF-562271 HCl purchased from Selleck.

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Biological Activity

Description PF-562271 HCl is the hydrochloride salt of PF-562271, which 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. Phase 1.
Features Dual FAK/Pyk2 inhibitor that has been tested in Phase I clinical trials for treatment of pancreatic, head and neck, and prostate cancers.
Targets
FAK [1]
()
PYK2 [1] CDK2/CyclinE [1] CDK3/CyclinE [1] CDK1/CyclinB [1]
1.5 nM 13 nM 30 nM 47 nM 58 nM
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. [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] PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. [4] 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. [5]

Protocol

Animal Research:[1]
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  • Animal Models: Athymic female mice bearing BxPc3 or PC3-M xenografts.
  • Formulation: 5% Gelucire
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (183.84 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 543.95
Formula

C21H21ClF3N7O3S

CAS No. 939791-41-0
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID