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PF-573228
PF-573228 是一種ATP競爭性的FAK抑制劑，無細胞試驗中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
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信號通路化合物庫 FDA抗癌藥物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | PF-573228 是一種ATP競爭性的FAK抑制劑，無細胞試驗中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。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | PF 573228作用于REF52 細胞, PC3 細胞, SKOV-3 細胞, 及L3.6p1 和 F-G, MDCK細胞，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，卻不抑制細胞生長或凋亡。PF 573228處理細胞，抑制血清或FN-定向遷移，且降低粘著斑轉(zhuǎn)換。[1] | |||
|---|---|---|---|---|
| 激酶實驗 | 親和測定 | |||
| 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 | ||||
| 細胞實驗 | 細胞系 | REF52 或 PC3 細胞 | ||
| 濃度 | ~10 μM | |||
| 孵育時間 | 3 天 | |||
| 方法 | REF52或PC3細胞按每孔1×104接種在24孔板中，一式三份，24小時后，使用指定濃度的每種抑制劑處理，進行生長實驗，持續(xù)3天。隨后，收集細胞并計數(shù)。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | 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胞缺失FAK有關(guān)[2]。 | |
|---|---|---|
化學(xué)信息&溶解度
| 分子量 | 491.49 | 分子式 | C22H20F3N5O3S |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 26 mg/mL ( (52.9 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(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.
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