PF-573228

製品コードS2013 バッチS201306

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	14 mg/mL (28.48 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-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, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 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 PF-573,228 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 each inhibitor 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

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：

Non-catalytic role of phosphoinositide 3-kinase in mesenchymal cell migration through non-canonical induction of p85β/AP2-mediated endocytosis [ Nat Commun, 2024, 15(1):2612]	PubMed: 38521786
Carboxymethyl chitosan-alginate enhances bone repair effects of magnesium phosphate bone cement by activating the FAK-Wnt pathway [ Bioact Mater, 2023, 20:598-609]	PubMed: 35846837
Mutant p53 sustains serine-glycine synthesis and essential amino acids intake promoting breast cancer growth [ Nat Commun, 2023, 14(1):6777]	PubMed: 37880212
The Tumor Suppressor DAB2IP Is Regulated by Cell Contact and Contributes to YAP/TAZ Inhibition in Confluent Cells [ Cancers (Basel), 2023, 15(13)3379]	PubMed: 37444489
Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adh Migr, 2023, 17(1):1-14]	PubMed: 36944577
Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adhesion & Migration, 2023, 17(1)]	PubMed: None
Phosphatidylserine released from apoptotic cells in tumor induces M2-like macrophage polarization through the PSR-STAT3-JMJD3 axis [ Cancer Commun (Lond), 2022, 42(3):205-222]	PubMed: 35191227
Wnt5a-Vangl1/2 signaling regulates the position and direction of lung branching through the cytoskeleton and focal adhesions [ PLoS Biol, 2022, 20(8):e3001759]	PubMed: 36026468
Fibrillin-1-regulated miR-122 has a critical role in thoracic aortic aneurysm formation [ Cell Mol Life Sci, 2022, 79(6):314]	PubMed: 35606547
Starvation mediates pancreatic cancer cell sensitivity to ferroptosis via ERK1/2, JNK and changes in the cell mesenchymal state [ Int J Mol Med, 2022, 49(6)84]	PubMed: 35514314

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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