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
CAS: 869288-64-2
产品质控
批次：
纯度：
99.92%
99.92
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 | ||
| 点击查看更多细胞系数据 | |||||
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 |
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| 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] | |||
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| 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。 |
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| 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 |
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30761269 | |
| Immunofluorescence | FAK / F-actin Emerin |
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30761269 | |
| Growth inhibition assay | Cell viability |
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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) | |||
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体外溶解度 |
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 |
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体内溶解配方 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
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
只
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，注：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：取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：取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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