PF-562271 (VS-6062)

製品コードS2890 バッチS289009

化学情報

	Synonyms	PF-00562271	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₂₀F₃N₇O₃S
	分子量	507.49	CAS No.	717907-75-0
Solubility (25°C)*	体外	DMSO	100 mg/mL (197.04 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PF-562271 (PF-00562271) は、強力なATP競合性可逆的FAK阻害剤であり、セルフリーアッセイにおけるIC50は1.5 nMです。Pyk2に対してはFAKよりも約10倍低く、一部のCDKを除き、他のプロテインキナーゼに対しては100倍以上の選択性を示します。
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. This compound is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. It (3.3 µM) results in G1 arrest of PC3-M cells. This chemical (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. It potently blocks blood vessel sprouting without detectable changes in vascular leakage. It (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. This compound (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. It (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. This chemical (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. It (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. This compound (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. It (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.

製品説明

PF-562271 (PF-00562271) は、強力なATP競合性可逆的FAK阻害剤であり、セルフリーアッセイにおけるIC50は1.5 nMです。Pyk2に対してはFAKよりも約10倍低く、一部のCDKを除き、他のプロテインキナーゼに対しては100倍以上の選択性を示します。

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. This compound is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. It (3.3 µM) results in G1 arrest of PC3-M cells.

This chemical (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. It potently blocks blood vessel sprouting without detectable changes in vascular leakage.

It (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. This compound (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. It (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts.

This chemical (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. It (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement.

This compound (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model.

It (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.

プロトコル(参考用のみ)

キナーゼアッセイ	Recombinant kinase assay
キナーゼアッセイ	Purified-activated FAK kinase domain (410–689 aa) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl₂ for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 mol/L H2SO4). IC50 values are determined using the Hill-Slope Model.
細胞アッセイ	細胞株	Cell-free assays
	濃度	IC50 of 1.5 and 14 nM for FAK and Pyk2 catalytic activity, respectively
	反応時間
	実験の流れ
動物実験	動物モデル	Athymic female mice bearing BxPc3 or PC3-M xenografts.
	投薬量	50 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/18339875/
https://pubmed.ncbi.nlm.nih.gov/18677107/
https://pubmed.ncbi.nlm.nih.gov/21045155/

https://pubmed.ncbi.nlm.nih.gov/20495381/
https://pubmed.ncbi.nlm.nih.gov/18348298/

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カスタマーフィードバック

: Data from [Environ Toxicol Pharmacol, 2014, 39(1), 114-124]

: Data from [PLoS One, 2014, 9(2), e88587]

: Data from [Data independently produced by , , Science, 2017, 9(420), doi: 10.1126/scitranslmed.aal3765]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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