PF-562271

製品コードS2890 バッチS289008

印刷

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 (warmed with 50ºC water bath)

100 mg/mL (197.04 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
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. ^[1] 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. ^[2] It (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. 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. ^[1] 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. ^[3] This compound (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. ^[4] 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. ^[5]

製品説明

PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

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. ^[1]

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. ^[2]

It (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. 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. ^[1]

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. ^[3]

This compound (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. ^[4]

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. ^[5]

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/

+ 展开

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Cytoskeletal activation of NHE1 regulates mechanosensitive cell volume adaptation and proliferation [ Cell Rep, 2024, 43(12):114992]	PubMed: 39579355
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Integrin signaling is critical for myeloid-mediated support of T-cell acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):6270]	PubMed: 37805579
Integrin signaling is critical for myeloid-mediated support of T-cell acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):6270]	PubMed: 37805579
VE-Cadherin modulates β-catenin/TCF-4 to enhance Vasculogenic Mimicry [ Cell Death Dis, 2023, 14(2):135]	PubMed: 36797281
VE-Cadherin modulates β-catenin/TCF-4 to enhance Vasculogenic Mimicry [ Cell Death Dis, 2023, 14(2):135]	PubMed: 36797281
Architecture of androgen receptor pathways amplifying glucagon-like peptide-1 insulinotropic action in male pancreatic β cells [ Cell Rep, 2023, 42(5):112529]	PubMed: 37200193
Combination of FAK inhibitor and cytokine-induced killer cell therapy: An alternative therapeutic strategy for patients with triple-negative breast cancer [ Biomed Pharmacother, 2023, 163:114732]	PubMed: 37254289

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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