PF-573228

製品コードS2013 バッチS201303

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₂₀F₃N₅O₃S

分子量

491.49

CAS No.

869288-64-2

Solubility (25°C)*

体外

DMSO

26 mg/mL (52.9 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-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
in vitro	PF 573228 blocks the phosphorylation of FAK Tyr³⁹⁷ in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, this compound (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with this chemical resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover. ^[1]
in vivo	Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with this compound did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice ^[2].

プロトコル(参考用のみ)

キナーゼアッセイ	Affinity determination
キナーゼアッセイ	Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl₂) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3
細胞アッセイ	細胞株	REF52 or PC3 cells
	濃度	~10 μM
	反応時間	3 days
	実験の流れ	Growth assays are performed by seeding 1 × 10⁴ REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of this compound for 3 days. Subsequently, the cells are harvested and counted.
動物実験	動物モデル	Ctrl-MT and MFCKO-MT mice
	投薬量	5 mg/kg
	投与方法	oral administration

参考

http://www.ncbi.nlm.nih.gov/pubmed?term=17395594
https://pubmed.ncbi.nlm.nih.gov/21471206/

カスタマーフィードバック

: Data from [PLoS One, 2014, 9(2), e88588]

: , 2014, Dr.Milica Pesic from Institute for Biological Research

: , , Nature, 2016, 537(7620):422-429.

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：

Galectin-3-integrin α5β1 phase separation disrupted by advanced glycation end-products impairs diabetic wound healing in rodents [ Nat Commun, 2025, 16(1):7287]	PubMed: 40775187
The essential clathrin adapter protein complex-2 is tumor suppressive specifically in vivo [ Nat Commun, 2025, 16(1):2254]	PubMed: 40050266
Combined inhibition of focal adhesion kinase and RAF/MEK elicits synergistic inhibition of melanoma growth and reduces metastases [ Cell Rep Med, 2025, 6(2):101943]	PubMed: 39922199
Mechanobiological mechanism of cyclic stretch-induced cell columnarization [ Cell Rep, 2025, 44(5):115662]	PubMed: 40338742
LATS1/2 inactivation in the mammary epithelium drives the evolution of a tumor-associated niche [ EMBO Rep, 2025, 10.1038/s44319-025-00370-3]	PubMed: 39953252
Urothelial collective-gliding response acts as a toll-like receptor 4-associated defense mechanism [ iScience, 2025, 28(10):113553]	PubMed: 41079633
Fibulin-4 and latent-transforming growth factor beta-binding protein-4 interactions with syndecan-2 and syndecan-3 are required for elastogenesis [ FASEB J, 2025, 39(7):e70505]	PubMed: 40168061
LIPUS promotes osteogenic differentiation of rat BMSCs and osseointegration of dental implants by regulating ITGA11 and focal adhesion pathway [ BMC Oral Health, 2025, 25(1):22]	PubMed: 39755586
The role of focal adhesion kinase in bladder cancer: translation from in vitro to ex vivo human urothelial carcinomas [ Radiol Oncol, 2025, 59(3):349-367]	PubMed: 40959921
Focal Adhesion Kinase Drives Rho/ROCK and mTOR Signaling to Protect and Augment Aortic Dissections [ JACC Basic Transl Sci, 2025, 10(9):101353]	PubMed: 40753710

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。