PF-573228

For research use only. Not for use in humans.

目录号:S2013

PF-573228 Chemical Structure

CAS No. 869288-64-2

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1562.28 现货
RMB 1201.44 现货
RMB 4669.29 现货
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客户使用Selleck生产的PF-573228发表文献50篇:

产品安全说明书

FAK抑制剂选择性比较

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A431 NVvUZXhmU2mwYYPlJIF{e2G7 MnTZglExKM7:TR?= MnPYSG1UVw>? NXfnTZNucW6qaXLpeJMhTkGNIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNVEhdk1? M{XXdVE4Ozl3NUm0
REF52 M1vEZmtqdmG|ZTDhd5NigQ>? M1;rbZ4yOCEQvF2= Mn7SSG1UVw>? Mki3bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kB,OTByIH7N M{nPT|E4Ozl3NUm0
PC3 NHyzenlMcW6jc3WgZZN{[Xl? NHfoZ2N,OTBizszN NFfMeW1FVVOR M2Kyb4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhOTByIH7N MnrQNVc{QTV3OUS=
SKOV-3 NW\qdXpMU2mwYYPlJIF{e2G7 NWn6T3lPhjFyIN88US=> M2DKZWROW09? NFPje4lqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIF\BT{BVgXJ|OUege4l1cCCLQ{WwJI9nKDVyIH7N NHrKbpcyPzN7NUW5OC=>
L3.6p1 NX7QUlkzU2mwYYPlJIF{e2G7 M1HnPZ4yOCEQvF2= M1X3PWROW09? MXTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFMxOCCwTR?= NXjPXWtVOTd|OUW1PVQ>
F-G M1H6XWtqdmG|ZTDhd5NigQ>? MlTiglExKM7:TR?= MYPEUXNQ NV\ISlZ4cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB|MDDuUS=> MXmxO|M6PTV7NB?=
MDCK NV;4Vm5NU2mwYYPlJIF{e2G7 NUe0eJFuhjFyIN88US=> M13rdWROW09? M3r2cIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiRlHLJHR6ejN7NzD3bZRpKEmFNUCgc4YhPTByIH7N NYXrdFZXOTd|OUW1PVQ>
PC3 MV3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXqxNEDPxE1? MnnjSG1UVw>? NGfxZ2F{cWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToMi=> M3v2Z|E4Ozl3NUm0
REF52 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{fEUFExKM7:TR?= NXf2N4pyTE2VTx?= Mn;nd4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJIdzd3e2aD6= NYL1T4piOTd|OUW1PVQ>
MDCK NXvTR20ySXCxcITvd4l{KGG|c3H5 MlW1NVAh|ryP NUP4RZhlTE2VTx?= MUTpcoR2[2W|IHHwc5B1d3Orcx?= MkS2NVc{QTV3OUS=
REF52 NUTGbHA6SXCxcITvd4l{KGG|c3H5 MnHoNVAh|ryP MUnEUXNQ NUPnW24{cW6mdXPld{BieG:ydH;zbZM> NVHXS3RGOTd|OUW1PVQ>
REF52 MYrGeY5kfGmxbjDhd5NigQ>? NEHTSYoyOCEQvF2= MYnEUXNQ M{e0dIJtd2OtczDz[ZJ2dSCjbnSgSm4ue3SrbYXsZZRm\CCvaXfyZZRqd25? NXPkSIxbOTd|OUW1PVQ>
platelet NF:1RXJHfW6ldHnvckBie3OjeR?= M4HIeVEh|ryP MoLuSG1UVw>? NYTxU|k4cW6qaXLpeJMheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJJNxemWjZHnu[y=> M3\0XlE6PzF4OECz
platelet MkH6SpVv[3Srb36gZZN{[Xl? MlvVNUDPxE1? M{GyOGROW09? M13XeYxm[WS|IITvJIlvcGmkaYTpc44hd2ZiUFHLJIFv\CCDS2S= MoP1NVk4OTZ6MEO=
platelet MkLKSpVv[3Srb36gZZN{[Xl? NV\xc5ZmOSEQvF2= MUXEUXNQ M1fxdoJtd2OtczDjZYxkcXWvIH3vZoltcXqjdHnvckBidmRiZHXud4Uh\3KjboXs[UB{\WO{ZYTpc44> NHrQdJMyQTdzNkiwNy=>
4T1 MWXGeY5kfGmxbjDhd5NigQ>? NHTvbWpFVVOR NWHZXooy[WKxbHnzbIV{KHSqZTDpcpRmemGldHnvckBj\XS5ZXXuJO6zOyCrboTl[5JqdiCjbnSgWO6zWi2LSR?= M3fSN|E6PzRyNEOz
MCF7 NV\ubIlEU2mwYYPlJIF{e2G7 MoWxglExKM7:TR?= MkDuSG1UVw>? NWrvTZVpcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDGRWshXHm{M{m3JJdqfGhiSVO1NEBw\iB2M{Cgcm0> Mn;6NlA{PTR5OEC=
TamR MVnLbY5ie2ViYYPzZZk> MUT+NVAh|ryP NIq5NGxFVVOR Mn\ObY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCIQVugWJlzOzl5IIfpeIghUUN3MDDv[kA2OCCwTR?= MViyNFM2PDd6MB?=
FasR NHu3OIpMcW6jc3WgZZN{[Xl? NXfMZ4RJhjFyIN88US=> NULGU2FrTE2VTx?= MUPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKE[DSzDUfZI{QTdid3n0bEBKSzVyIH;mJFE{OCCwTR?= M1jkWlIxOzV2N{iw
TamR NEfXb2JHfW6ldHnvckBie3OjeR?= M2fnTFEh|ryP NGLJTmNFVVOR NFHDfIxqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MkXDNlA{PTR5OEC=
FasR NY\JN442TnWwY4Tpc44h[XO|YYm= M{m5cVEh|ryP NH;0UVJFVVOR NUTHW3pucW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MUmyNFM2PDd6MB?=
endothelial cell NETZOGFMcW6jc3WgZZN{[Xl? NE\BNYs1OCCwTR?= MnO0SG1UVw>? M{n1dolvcGmkaYTzJGgzVzJvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRlHL NXP1TXV2OjF{MUK0NFI>
endothelial cell M1rSN2Z2dmO2aX;uJIF{e2G7 MVy0NEBvVQ>? NHjNdHVFVVOR NIexS|hqdmirYnn0d{BJOk9{LXnu[JVk\WRic4Ty[ZN{KG[rYnXyJIZwem2jdHnvci=> NF[wPI0zOTJzMkSwNi=>
endothelial cell M4jPRWFxd3C2b4Ppd{Bie3OjeR?= NV7WW2VMPDBibl2= M1T1e2ROW09? MWjpcohq[mm2czDhdI9xfG:|aYO= MW[yNVIyOjRyMh?=
GH3 M1vJ[2Z2dmO2aX;uJIF{e2G7 NIXS[5A{KM7:TR?= MULEUXNQ MnzHbY5kemWjc3XzJGlMMEOjKTDhcZBtcXS3ZHW= NIjnfJEzOTl{NUWxNi=>
GH3 NX\zVVh5TnWwY4Tpc44h[XO|YYm= MlnFN{DPxE1? NWP2VoFxTE2VTx?= M3T1UYVvcGGwY3XzJGJMS2FvY3jhco5mdCCjY4Tpeol1gQ>? MXyyNVkzPTVzMh?=
HUVEC NID3Z|RkgXSxdH;4bYNqfHliYYPzZZk> MXL+NVAh|ryP NVLIXYZsTE2VTx?= NEPDdZRqdXCjaYLzJIVv\G:2aHXsbYFtKGOnbHygeoli[mmuaYT5 M3i1[lIzODd3MEW3
HUVEC NEO0UFdMcW6jc3WgZZN{[Xl? NV\oRlF{PSEQvF2= M4n0d2ROW09? NFTidWhqdmirYnn0d{BHSUtia3nuZZNmKGGldHn2bZR6 M3m1NVIzODd3MEW3
HUVEC NFvCc5VHfW6ldHnvckBie3OjeR?= Mn7QOUDPxE1? NFSzd4JFVVOR MVjpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NIXMb4kzOjB5NUC1Oy=>
HUVEC MYLBdI9xfG:|aYOgZZN{[Xl? MYm1JO69VQ>? NVzDZWRkTE2VTx?= MkT0bY5lfWOnczDhdI9xfG:|aYO= MUOyNlA4PTB3Nx?=
HUVEC NW\hcFd5TnWwY4Tpc44h[XO|YYm= M{TCXFUh|ryP MUnEUXNQ NYDHbZMxcW2yZXTld{BmdmSxdHjlcIlidCClZXzsJI1q\3KjdHnvckBidmRiYXz0[ZJ{KHSqZTDj[YxtfWyjcjDhZ5RqdiCleYTvd4tmdGW2b36= M2XESVIzODd3MEW3
HUVEC Moi3SpVv[3Srb36gZZN{[Xl? M4T4OVUh|ryP NUW0[4RnTE2VTx?= M3rYXYJtd2OtczDIWXZGSyC|cILveZRqdmdib36gZ49tdGGpZX6gTUBo\Wy| M3e0W|IzODd3MEW3
human peripheral blood T cells NYTwS3pnU2mwYYPlJIF{e2G7 Mn7YglExKM7:TR?= NF\xeZdFVVOR NWXUT|lkcW6qaXLpeJMhe2m2ZT3zdIVkcW[rYzDwbI9{eGixconsZZRqd25ib3[gSmFM MUWyN|kzQDF6OB?=
human peripheral blood T cells NIfsfo5HfW6ldHnvckBie3OjeR?= MlnlglExKM7:TR?= MVTEUXNQ MYTpcZBicXK|IGTDVk1qdmS3Y3XkJHQh[2WubDDtc5JxcG:ub3fpZ4FtKGOqYX7n[ZMh[W6mIHHseIVzeyCjY4Tpeol1gSCxZjDSbI9C MoWyNlM6OjhzOEi=
human peripheral blood T cells MW\GeY5kfGmxbjDhd5NigQ>? M{DoZZ4yOCEQvF2= M2HtfGROW09? Mn3ObY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHpCWC15MDDhcoQhVEGW M2XMTFI{QTJ6MUi4
human peripheral blood T cells NGjYVFNHfW6ldHnvckBie3OjeR?= NXPU[WdphjFyIN88US=> NHrjXWZFVVOR NWnYTGdZcW2yYXnyd{BCdnSrZ3XuMYRmeGWwZHXueEBVKGOnbHygZ49vcnWpYYTpc44> NGDUeFkzOzl{OEG4PC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cyclin B1; 

PubMed: 30761269     


(D) On the third day, PF-573228-treated cells were harvested and subjected to Western blot analysis for cyclin B1. Cyclin B1 levels were much higher in A549 cells with 1 μM PF-573228 or without PF-573228 treatment than in the cells treated with higher concentrations of PF-573228. (E) After 10 μM PF-573228 treatment, cyclin B1 levels declined markedly in H460 cells. (F) PF-573228 administration slightly reduced cyclin B1 levels in H1299 cells. 

p-FAK / FAK ; 

PubMed: 30761269     


FAK expression levels and FAK activity, as measured by the phosphorylation of FAK at tyrosine 576 and 577, were quantified by Western blot analysis after treatment of lung cancer cells with PF-573228 for 3 days.

Lamin A / Lamin C; 

PubMed: 30761269     


(B) The cells treated with 10 μM PF-573228 exhibited a decrease in p-FAK levels. Lamin A and lamin C expression levels were much lower in A549 cells exposed to 10 μM PF-573228. 

30761269
Immunofluorescence
FAK / F-actin; 

PubMed: 30761269     


(B) The cells were stained with phalloidin to visualize F-actin (red) and a FAK antibody to visualize the FAK distribution (green). In cells without PF-573228 administration, FAK translocated to focal adhesions at the tips of actin stress fibers, and the focal adhesions were relatively large. When cells were exposed to 10 μM PF-573228, FAK translocation to focal adhesions was reduced, and the sizes of the focal adhesions were smaller. Nuclei in cells treated with PF-573228 were deformed, as visualized with DAPI staining, whereas most nuclei in cells without PF-573228 treatment were oval shaped. 

Emerin; 

PubMed: 30761269     


(A) After PF-573228 treatment of A549 cells, the cells were fixed and stained with phalloidin to label F-actin (red) and an antibody against emerin (green) to outline the nuclear shape. Cells treated with PF-573228 were extremely large and had deformed nuclei, whereas mostly oval-like nuclei were present in the cells without PF-573228 treatment. 

30761269
Growth inhibition assay
Cell viability; 

PubMed: 30761269     


Three different types of lung cancer cells, (A) A549 lung adenocarcinoma and (B) H460, and (C) H1299 large cell carcinoma, were selected for the PF-573228 administration regimen. Cell growth curves of the three lung cancer cell lines treated with various doses of PF-573228 for 4 days were established. The administration of PF-573228 at 10 μM to the lung cancer cells effectively suppressed cell growth in vitro, as proliferative activity totally ceased in the cells exposed to 10 μM PF-573228.

30761269
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

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:

[1]

- 合并
  • Cell lines: REF52 或 PC3 细胞
  • Concentrations: ~10 μM
  • Incubation Time: 3 天
  • Method:

    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。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: Ctrl-MT 和 MFCKO-MT 小鼠
  • Dosages: 5 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 26 mg/mL (52.9 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+2% Tween 80+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 491.49
化学式

C22H20F3N5O3S

CAS号 869288-64-2
储存条件 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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.

FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID