PF-573228

目錄號(hào)：S2013 Purity: 99.92%

PF-573228 是一種ATP競爭性的FAK抑制劑，無細(xì)胞試驗(yàn)中IC50為4 nM，作用于FAK比作用于Pyk2，CDK1/7 和 GSK-3β選擇性高~50到250倍。PF-573228 可誘導(dǎo)凋亡。

PF-573228 Chemical Structure

CAS: 869288-64-2

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1562.28	現(xiàn)貨
10mg	1201.44	現(xiàn)貨
50mg	4669.29	現(xiàn)貨
1g	32678.1	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.92%

99.92

PF-573228相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	PF-562271 Defactinib (VS-6063) VS-4718 (PND-1186) PF-562271 HCl PF-562271 Besylate TAE226 (NVP-TAE226) GSK2256098 PF-431396 Y15	點(diǎn)擊展開
相關(guān)化合物庫	酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫血管生成相關(guān)化合物庫 HIF-1信號(hào)通路化合物庫 FDA抗癌藥物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	活性描述	文獻(xiàn)信息
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

FAK ^[1]
(Cell-free assay)

4 nM

體外研究(In Vitro)
體外研究活性	PF 573228作用于REF52 細(xì)胞, PC3 細(xì)胞, SKOV-3 細(xì)胞, 及L3.6p1 和 F-G, MDCK細(xì)胞，抑制FAK Tyr³⁹⁷磷酸化，IC50為30-500 nM。然而, PF 573228 (1 μM) 抑制80% FAK磷酸化，卻不抑制細(xì)胞生長或凋亡。PF 573228處理細(xì)胞，抑制血清或FN-定向遷移，且降低粘著斑轉(zhuǎn)換。^[1]
激酶實(shí)驗(yàn)	親和測定
激酶實(shí)驗(yàn)	純化的激活FAK激酶結(jié)構(gòu)域（410-689氨基酸）與50 μM ATP, 和每孔 10 μg Glu和Tyr的隨機(jī)肽 (摩爾比為4:1), 聚(Glu/Tyr) 在激酶緩沖液(50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl₂) 中反應(yīng)15分鐘。使用按1/2-Log濃度連續(xù)稀釋的化合物（起始于1 μM的最高濃度）處理磷酸化的聚(Glu/Tyr)。每種濃度按一式三份進(jìn)行。使用一般的抗磷酸化酪氨酸（PY20）抗體，隨后使用辣根過氧化物酶偶聯(lián)的山羊抗小鼠IgG抗體檢測聚(Glu/Tyr)的磷酸化。加入標(biāo)準(zhǔn)的辣根過氧化物酶底物3,3
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	REF52 或 PC3 細(xì)胞
	濃度	~10 μM
	孵育時(shí)間	3 天
	方法	REF52或PC3細(xì)胞按每孔1×10⁴接種在24孔板中，一式三份，24小時(shí)后，使用指定濃度的每種抑制劑處理，進(jìn)行生長實(shí)驗(yàn)，持續(xù)3天。隨后，收集細(xì)胞并計(jì)數(shù)。
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在Ctrl-MT小鼠中，通過PF-573228抑制FAK能顯著地抑制乳腺腫瘤的發(fā)生以及肺癌的轉(zhuǎn)移。相反地，用PF-573228處理MFCKO-MT小鼠則不影響乳腺腫瘤的發(fā)生，這可能與這些小鼠中乳腺上皮細(xì)胞缺失FAK有關(guān)^[2]。

參考文獻(xiàn)
[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.

參考文獻(xiàn)

[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.

化學(xué)信息&溶解度

分子量	491.49	分子式	C₂₂H₂₀F₃N₅O₃S
CAS號(hào)	869288-64-2	SDF	Download PF-573228 SDF
Smiles	CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 26 mg/mL ( (52.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 98 mg/mL ( (199.39 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : Insoluble ( ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 26 mg/mL ( (52.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 14 mg/mL ( (28.48 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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):

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PF-573228

產(chǎn)品質(zhì)控

PF-573228相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持

常見問題及建議解決方法