PF-573228

製品コード：S2013 純度：99.92%

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.

CAS No. 869288-64-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 28500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 85500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（87）

製品安全説明書

現在のバッチを見る：純度： 99.92%

99.92

PF-573228関連製品

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関連化合物ライブラリー	Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Angiogenesis Related compound Library HIF-1 Signaling Pathway Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

FAKシグナル伝達経路

FAK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	活性情報	PMID
FasR	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 130 nM	20354780
TamR	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM	20354780
MCF7	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 430 nM	20354780
platelet	Function assay	1 μM	blocks calcium mobilization and dense granule secretion	19716803
platelet	Function assay	1 μM	leads to inhibition of PAK and AKT	19716803
platelet	Function assay	1 μM	inhibits platelet aggregation and spreading	19716803
REF52	Function assay	10 μM	blocks serum and FN-stimulated migration	17395594
REF52	Apoptosis assay	10 μM	induces apoptosis	17395594
MDCK	Apoptosis assay	10 μM	induces apoptosis	17395594
REF52	Growth inhibitory assay	10 μM	significantly inhibits cell growth.	17395594
PC3	Growth inhibitory assay	10 μM	significantly inhibits cell growth.	17395594
MDCK	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 500 nM	17395594
F-G	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 30 nM	17395594
L3.6p1	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 300 nM	17395594
SKOV-3	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM	17395594
PC3	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of 100 nM	17395594
REF52	Kinase assay	~10 μM	inhibits the phosphorylation of FAK Tyr397 with IC50 of ~100 nM	17395594
A431	Kinase assay	~10 μM	inhibits FAK phosphorylation with IC50 of 11 nM	17395594
TamR	Function assay	1 μM	inhibits cell migration	20354780
FasR	Function assay	1 μM	inhibits cell migration	20354780
endothelial cell	Kinase assay	40 nM	inhibits H2O2-induced phosphorylation of FAK	21212402
endothelial cell	Function assay	40 nM	inhibits H2O2-induced stress fiber formation	21212402
endothelial cell	Apoptosis assay	40 nM	inhibits apoptosis	21212402
GH3	Function assay	3 μM	increases IK(Ca) amplitude	21925512
GH3	Function assay	3 μM	enhances BKCa-channel activity	21925512
HUVEC	cytotoxicity assay	~10 μM	impairs endothelial cell viability	22075057
HUVEC	Kinase assay	5 μM	inhibits FAK kinase activity	22075057
HUVEC	Function assay	5 μM	induces cell cycle arrest	22075057
HUVEC	Apoptosis assay	5 μM	induces apoptosis	22075057
HUVEC	Function assay	5 μM	impedes endothelial cell migration and alters the cellular actin cytoskeleton	22075057
HUVEC	Function assay	5 μM	blocks HUVEC sprouting on collagen I gels	22075057
human peripheral blood T cells	Kinase assay	~10 μM	inhibits site-specific phosphorylation of FAK	23928188
human peripheral blood T cells	Function assay	~10 μM	impairs TCR-induced T cell morphological changes and alters activity of RhoA	23928188
human peripheral blood T cells	Function assay	~10 μM	inhibits phosphorylation of ZAP-70 and LAT	23928188
human peripheral blood T cells	Function assay	~10 μM	impairs Antigen-dependent T cell conjugation	23928188
4T1	Function assay		abolishes the interaction between β3 integrin and TβR-II	19740433
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
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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.

Targets

FAK ^[1]
(Cell-free assay)

4 nM

In Vitro
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]
Kinase Assay	Affinity determination
Kinase Assay	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
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	cyclin B1 p-FAK / FAK Lamin A / Lamin C		30761269
	Immunofluorescence	FAK / F-actin Emerin		30761269
	Growth inhibition assay	Cell viability		30761269

In Vivo
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].
動物実験	動物モデル	Ctrl-MT and MFCKO-MT mice
	投与量	5 mg/kg
	投与経路	oral administration

参考
[1] Slack-Davis JK, et al. J Biol Chem, 2007, 282(20), 14845-14852. [2] Fan H, et al. J Biol Chem. 2011, 286(21):18573-82.

参考

化学情報

分子量	491.49	化学式	C₂₂H₂₀F₃N₅O₃S
CAS No.	869288-64-2	SDF	Download PF-573228 SDFをダウンロードする
Smiles	CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 26 mg/mL ( (52.9 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問（FAQ）

質問1:
Would you please let me know the detail of how to dissolve PF-573228 (Catalog No.S2013) for in vivo study (oral administration)?

回答
PF-573228 in 30% PEG400+0.5% Tween80+ 5% Propylene glycol at 30mg/ml is a suspension. If you will use the compound for oral gavage, this suspension is fine for it.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):