PF-562271

For research use only. Not for use in humans.

目录号:S2890 别名: PF-00562271

PF-562271 Chemical Structure

CAS No. 717907-75-0

PF-562271 (PF-00562271)是一种有效的,ATP竞争性的,可逆的FAK抑制剂,无细胞试验中IC50为1.5 nM,作用于FAK比作用于Pyk2选择性高10倍左右,比作用于其他蛋白激酶(除了一些CDKs)选择性高100倍以上。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2862.96 现货
RMB 1392.84 现货
RMB 2194.82 现货
RMB 5469.68 现货
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客户使用Selleck生产的PF-562271发表文献91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-562271 (PF-00562271)是一种有效的,ATP竞争性的,可逆的FAK抑制剂,无细胞试验中IC50为1.5 nM,作用于FAK比作用于Pyk2选择性高10倍左右,比作用于其他蛋白激酶(除了一些CDKs)选择性高100倍以上。
靶点
FAK [1]
(Cell-free assay)
PYK2 [1]
(Cell-free assay)
CDK2/CyclinE [1]
(Cell-free assay)
CDK3/CyclinE [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
1.5 nM 13 nM 30 nM 47 nM 58 nM
体外研究

PF-562271会结合到ATP与FAK结合的部位,在激酶铰链区形成抑制剂与主链原子之间的两种氢键。PF-562271在测量FAK磷酸化可诱导的基于细胞的分析中效果很好,IC50为5 nM。PF-562271 (3.3 μM)导致PC3-M细胞周期停滞在G1期[1]。在鸡胚绒毛尿囊膜实验中PF-562271 (1nM)阻断bFGF刺激的血管生成。 PF-262271 强有效的阻断血管生长但对血管渗漏没有明显影响[2]。PF-562271 (250 nM)可以完全抑制整体A431 细胞侵入胶原蛋白中[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IST-MES1 NWjZUJg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTR7Lki5OFQh|ryP NIT6VG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
EKVX NVq1So8zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i3U2lEPTB;NEmuOlc{OSEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1395 NF\6fYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HRUWlEPTB;NEmuNFQ6OiEQvF2= NX:4O3Y1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
LS-1034 NF\Cb25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HaeWlEPTB;NEiuPFk2PCEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
RT4 NXzhOpVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlKzTWM2OD12OD64N|c4KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
PSN1 M3j3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTR6LkG0NFEh|ryP NFHQ[nU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
KY821 NVK0R4J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz4SGtIUUN3ME20O{43PDN2IN88US=> NGHnXYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
LC-1F MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnoNHdsUUN3ME20O{43OTB3IN88US=> NH64TXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
Saos-2 M3LuZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTGdVV3UUN3ME20O{4{OTJ|IN88US=> M332N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
BL-70 M2Ho[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTR4Lke3N|ch|ryP MmW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
HCC1569 NYXMbYx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLsWmZVUUN3ME20Ok42QTF5IN88US=> NX;sVY55RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
CP66-MEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF33VGVKSzVyPUS2MlI4QDlizszN MkTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NCI-H187 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTR4LkG4Olkh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H1703 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjCbZFKSzVyPUS2MlA2QTJizszN MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H2342 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnqyTWM2OD12NT6xNVE4KM7:TR?= MoPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
EoL-1-cell NVzpXXh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXkTWM2OD12ND65NVM3KM7:TR?= NH:4[289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
MRK-nu-1 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1mwPWlEPTB;NESuO|QyPCEQvF2= M2HNNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
SAS MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHyTWM2OD12Mz60Nlg5KM7:TR?= NVn0NohJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
LB996-RCC NGXoWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTR{LkiwNFgh|ryP NYXjPWNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
OAW-42 NYq4ZYlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDhPY5KSzVyPUSyMlI6PDJizszN M1faSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
PF-382 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHuXohKSzVyPUSwMlc1QDdizszN M{PF[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
COLO-678 MmTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u5VWlEPTB;NECuOVk2KM7:TR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
NCI-H2170 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN7Lkm5O|ch|ryP MnK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KU-19-19 NFW5PY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPxTWM2OD1|OT62NlgzKM7:TR?= M1;mZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
SW756 M2K0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTN7LkWwPVEh|ryP M1vF[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
Capan-2 Mnf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;rSGlEPTB;M{muNFUxQSEQvF2= MljEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
MDA-MB-453 NGXjUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTN7LkCyNVgh|ryP NVjkd4RPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB6NEW0Ok8oRlODTlfFVlww[T5?
TGBC24TKB NYC2T4tFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXlTWM2OD1|OD6wNlM6KM7:TR?= NEjvO4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
A375 MlHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f1UWlEPTB;M{euO|Y1PyEQvF2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
RCM-1 NU\XSpk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN5LkWzOVgh|ryP MnPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
KARPAS-422 Ml\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ToPWlEPTB;M{euOFQ{OSEQvF2= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
LNCaP-Clone-FGC NWjTVndMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHuTWM2OD1|Nz6xPVA{KM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
HCC1937 M{DZRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q4VWlEPTB;M{euNFE2PCEQvF2= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
no-11 M4\1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN4Lki1N|Yh|ryP NG[0UXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
KYSE-140 NYK4[YV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHQW3FKSzVyPUO2MlczQThizszN NIrzdFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh2NUS2M{c,W0GQR1XSQE9iRg>?
SW1463 MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL1bIlKSzVyPUO2MlY2PjZizszN MnnXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
NEC8 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPDeplKSzVyPUO2MlQ6OjRizszN MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
BV-173 NGjNUXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz4N4dKSzVyPUO1MlgzPjRizszN M2DUbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
NCI-H1355 NV7KfJUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfNNYJzUUN3ME2zOU44PzF6IN88US=> MonqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5PDV2Nj:nQnNCVkeHUkyvZV4>
EFE-184 NFvONnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\STmlEPTB;M{WuOlgzQSEQvF2= M{PwZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
HH NYPZNIR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XDW2lEPTB;M{WuOFE1OSEQvF2= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFg1PTR4Lze+V2FPT0WUPD;hQi=>
HC-1 NGfXWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTCTWM2OD1|NT60NFI1KM7:TR?= M3qwflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQDR3NE[vK|5USU6JRWK8M4E,
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MG 63 (6-TG R) NUjubIdHeUiWUzDhd5NigQ>? M17TTJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NYHnPZdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
wild type fibroblast cells NUXMe5A6eUiWUzDhd5NigQ>? Mm\6dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKGOxboTyc4whUGhid3ns[EB1gXCnIH\pZpJw[myjc4SgZ4VtdHN? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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A673 NVqyb|FoeUiWUzDhd5NigQ>? NVXDT|E5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? NYq5VYU1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 MYHxTHRUKGG|c3H5 MlzhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOTJiY3XscJM> M3v0[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 M33RfJFJXFNiYYPzZZk> MnHLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUGFPNTViY3XscJM> NYmyblBiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY NFLB[nNyUFSVIHHzd4F6 NYDHVGk1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? Mo\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 M37Ze5FJXFNiYYPzZZk> NWOwUo5HeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? NGOwUJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
U-2 OS NEDibnlyUFSVIHHzd4F6 Ml;CdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ NEfTepo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M1v4NJFJXFNiYYPzZZk> MmXqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=> NVXNdVFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NGnsXnJyUFSVIHHzd4F6 NYq5SWh[eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NFzWXXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 MWPxTHRUKGG|c3H5 M3rB[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG9JWy13MDDj[Yxtew>? NIrT[XI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NXPN[ZVZeUiWUzDhd5NigQ>? NVzkR2NCeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= M2nJOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-FAK / FAK / p-Talin / Talin ; 

PubMed: 26530902     


Dose response of PF-562271 on the phosphorylation of FAK-Y397 or Talin-S425 in PC3-mm2 cells.

p-Src / Src / p-paxillin / Paxillin / ICAM-1 ; 

PubMed: 29417941     


MDA-MB-231 cells transfected with FAK-specific siRNAs or treated for 12 h with PF-562271 at the indicated concentrations were subjected to immunoblotting with indicated antibodies.

26530902 29417941
Immunofluorescence
p-FAK; 

PubMed: 26530902     


Immunostaining of PC3-mm2 cells showed that phosphorylated FAK is localized at focal adhesions (inset).

26530902
Growth inhibition assay
Cell viability; 

PubMed: 28953264     


MTT assay showed inhibition of cell proliferation and viability in HCT116 (B) and SW480 (D) cell lines treated with resveratrol and/or different concentrations of FAK-Inhibitor (PF-562271: 0.01, 0.1, 1, and 10 µM) cultured in monolayer for 12 h. Data shown are representative of three independent sets of experiments. Values were compared with the control and statistically significant values with p < 0.05 are designated by an asterisk (*) and p < 0.01 are designated by two asterisks (**).

28953264
体内研究 在携带U87MG的小鼠中PF-562271 (< 33 mg/kg 口服)抑制肿瘤中FAK磷酸化并具有时间和剂量依赖特性。PF-562271 (50 mg/kg, 口服,一天两次)对BxPc3异种移植小鼠中肿瘤生长抑制率为86% ,对PC3-M异种移植小鼠中肿瘤生长抑制率为45%。PF-562271 (25mg/kg, 一天两次)处理的携带H125肺部异种移植肿瘤凋亡率提高2倍[1]。 PF-562271 (33 mg/kg,口服)24小时后抑制小鼠中肿瘤细胞的广泛运动。PF-562271 (33 mg/kg, 口服)导致小鼠中E-cadherin动力学的改变,这与减弱的E-cadherin依赖的整体细胞运动有关 [3]。在皮下局部异种移植PC3M-luc-C6的小鼠模型中 PF-562271 (25 mg/kg, 口服,一天两次)导致肿瘤生长率62%的抑制[4]。在胫骨植入MDA-MB-231细胞的大鼠中PF-562271 (5mg/kg, 口服)导致骨钙素和松质骨参数显著而相似的增加同时导致肿瘤生长速度和骨愈合信号的下降[5]

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)

动物实验:[1]
- 合并
  • Animal Models: 携带BxPc3或 PC3-M异种移植的无胸腺雌性小鼠
  • Dosages: 50 mg/kg
  • Administration: 填喂给药
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL warmed (197.04 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+40% PEG 300+5% Tween 80+50% ddH2O
5 mg/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 507.49
化学式

C21H20F3N7O3S

CAS号 717907-75-0
储存条件 粉状
溶于溶剂
别名 PF-00562271

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

FAK Signaling Pathway Map

相关FAK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID