PF-573228

PF-573228 是一种ATP竞争性的FAK抑制剂,无细胞试验中IC50为4 nM,作用于FAK比作用于Pyk2,CDK1/7 和 GSK-3β选择性高~50到250倍。PF-573228 可诱导凋亡。

PF-573228 Chemical Structure

PF-573228 Chemical Structure

CAS: 869288-64-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1562.28 现货
10mg 1201.44 现货
50mg 4669.29 现货
1g 32678.1 现货
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PF-573228相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
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生物活性

产品描述 PF-573228 是一种ATP竞争性的FAK抑制剂,无细胞试验中IC50为4 nM,作用于FAK比作用于Pyk2,CDK1/7 和 GSK-3β选择性高~50到250倍。PF-573228 可诱导凋亡。
靶点
FAK [1]
(Cell-free assay)
4 nM
体外研究(In Vitro)
体外研究活性 PF 573228作用于REF52 细胞, PC3 细胞, SKOV-3 细胞, 及L3.6p1 和 F-G, MDCK细胞,抑制FAK Tyr397磷酸化,IC50为30-500 nM。然而, PF 573228 (1 μM) 抑制80% FAK磷酸化,却不抑制细胞生长或凋亡。PF 573228处理细胞,抑制血清或FN-定向迁移,且降低粘着斑转换。[1]
激酶实验 亲和测定
纯化的激活FAK激酶结构域(410-689氨基酸)与50 μM ATP, 和每孔 10 μg Glu和Tyr的随机肽 (摩尔比为4:1), 聚(Glu/Tyr) 在激酶缓冲液(50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) 中反应15分钟。使用按1/2-Log浓度连续稀释的化合物(起始于1 μM的最高浓度)处理磷酸化的聚(Glu/Tyr)。每种浓度按一式三份进行。使用一般的抗磷酸化酪氨酸(PY20)抗体,随后使用辣根过氧化物酶偶联的山羊抗小鼠IgG抗体检测聚(Glu/Tyr)的磷酸化。加入标准的辣根过氧化物酶底物3,3
细胞实验 细胞系 REF52 或 PC3 细胞
浓度 ~10 μM
孵育时间 3 天
方法

REF52或PC3细胞按每孔1×104接种在24孔板中,一式三份,24小时后,使用指定浓度的每种抑制剂处理,进行生长实验,持续3天。随后,收集细胞并计数。

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性 在Ctrl-MT小鼠中,通过PF-573228抑制FAK能显著地抑制乳腺肿瘤的发生以及肺癌的转移。相反地,用PF-573228处理MFCKO-MT小鼠则不影响乳腺肿瘤的发生,这可能与这些小鼠中乳腺上皮细胞缺失FAK有关[2]

化学信息&溶解度

分子量 491.49 分子式

C22H20F3N5O3S

CAS号 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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 26 mg/mL ( (52.9 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 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.

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