PD173074

For research use only. Not for use in humans.

Pfizer辉瑞授权 目录号:S1264

PD173074 Chemical Structure

CAS No. 219580-11-7

PD173074 是一种有效的FGFR1抑制剂,在无细胞试验中IC50约为25 nM,也能抑制VEGFR2,IC50为100-200 nM,作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 802.11 现货
RMB 575.36 现货
RMB 3867.14 现货
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客户使用Selleck生产的PD173074发表文献88篇:

产品安全说明书

FGFR抑制剂选择性比较

生物活性

产品描述 PD173074 是一种有效的FGFR1抑制剂,在无细胞试验中IC50约为25 nM,也能抑制VEGFR2,IC50为100-200 nM,作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。
靶点
FGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
~25 nM 100 nM-200 nM
体外研究

PD173074是FGFR1的ATP竞争性抑制剂, Ki约为40 nM。PD173074也是VEGFR2的有效抑制剂。相比FGFR1,PD173074弱抑制Src,INSR,EGFR,PDGFR,MEK和PKC的活性,IC 50值大1000倍以上。PD173074剂量依赖性地抑制FGFR1和VEGFR2的自身磷酸化,IC50 分别为1-5 nM和100-200 nM。[1] PD173074以剂量依赖的方式抑制FGF-2促进的颗粒神经元存活,IC50是12 nM,活性是SU 5402的1,000倍以上。[2] D173074特异性地抑制FGF-2-介导的少突胶质细胞(OL)谱系细胞的细胞增殖,分化和MAPK激活。[3] 在多发性骨髓瘤(MM)细胞系中,PD173074对野生受体和FGFR3突变有活性。PD173074还以剂量依赖的方式有效地抑制FGFR3的自磷酸化,IC50约为5 nM。PD173074有力地降低了表达FGFR3的KMS11细胞和KMS18细胞的活力,IC50小于20 nM。aFGF刺激的MM细胞生长受PD173074抑制是和FGFR3的表达高度相关的。PD173074完全抑制由Y373C FGFR3介导而不是的Ras介导的NIH 3T3转化,这表明PD173074专门针对FGFR3基因介导的细胞转化和缺乏非特异性的细胞毒性作用。PD173074也诱导KMS11和KMS18细胞功能成熟。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LQTmlEPTB;MD6wNVIzPSEQvF2= Mof5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
KG-1 NWjnTGRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HpUGlEPTB;MD6wOVEzQSEQvF2= NIq1SXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
MFM-223 NGnrWXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwMkG1O|Yh|ryP M4DaVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
EoL-1-cell NV;1N5h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P0cWlEPTB;MD6zNlk5PCEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
ECC10 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\sTWM2OD1yLkOzPFk5KM7:TR?= NULKTJB1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
H-EMC-SS M4PaO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzXTWM2OD1yLkO0O|E2KM7:TR?= M2nEclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
AN3-CA MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\pfZBMUUN3ME2wMlQxOTN|IN88US=> MmG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
HuO-3N1 MmLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XDUGlEPTB;MD61OFY2OyEQvF2= M{DOTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
RT-112 NXnN[FhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjXTWM2OD1yLkW0O|AyKM7:TR?= MnPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
NEC8 NVrYN3RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M125WmlEPTB;MD61OlI5QSEQvF2= NGnTUHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
D-263MG MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwN{GxOVkh|ryP NWrkO2hVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
SW962 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwN{i5PFgh|ryP MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
BV-173 M3q0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f0UGlEPTB;MD64OFYzOyEQvF2= NWDyTZJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
MFE-280 NVfhcGpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;FTWM2OD1yLki1PFczKM7:TR?= NH3uR4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
HuH-7 NUDVb5R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGj2UllKSzVyPUGuNlQ1PjRizszN MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
RS4-11 NIiwXldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHBSJBQUUN3ME2xMlM{QDh4IN88US=> NVSwXFdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
DMS-114 M4e2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7obWRKSzVyPUGuN|Y4OzdizszN M1u0fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
MSTO-211H Mo\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon5TWM2OD1zLkS3N|c5KM7:TR?= NX\PVHk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
DU-145 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfv[opWUUN3ME2xMlU5OjF5IN88US=> NYXQfpdDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
A172 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjYc4wzUUN3ME2xMlcxOzV3IN88US=> Ml35QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
SBC-1 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrMXFUxUUN3ME2yMlA6PCEQvF2= NVz6VW0xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
H9 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTaUHVxUUN3ME2yMlE1OzB4IN88US=> NYXwZ2tLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
NCI-SNU-1 NFWyXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTPW4pKSzVyPUKuNVg{QTRizszN NHPybFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
NCI-H720 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPYNWRKSzVyPUKuNlEzQDNizszN NGL4UWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
HCC2218 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnruTWM2OD1{LkO3PVM6KM7:TR?= NIOyPWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
G-401 NIexUGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnWcFJMUUN3ME2yMlQ4OTh7IN88US=> NFnabXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
MPP-89 NX60dms{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrxTWM2OD1{LkS4N|Y1KM7:TR?= NIrHc4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
697 M{PPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXTVoRKSzVyPUKuOlU{OzFizszN NWHJe5JPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
KARPAS-45 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7XPJFKSzVyPUKuO|A4PDdizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
MG-63 M2G0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzkTWM2OD1{Lkm0NlYzKM7:TR?= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
NTERA-S-cl-D1 NXPWWGJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jS[GlEPTB;Mz6wN|Q4OiEQvF2= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
G-402 MkLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nscmlEPTB;Mz6xNlczPyEQvF2= MnflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
NKM-1 Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;ZNpZKSzVyPUOuNVM2PjRizszN MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
RH-18 M{\XRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTNwMUm1PVgh|ryP MofuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
NCI-H1092 M3vCfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTNwMUm2PUDPxE1? NGP1SWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
RPMI-8226 NHPQW3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\XTWM2OD1|LkKzOFQ4KM7:TR?= NHLFRmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
GAMG NWTTSlF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn4NGF4UUN3ME2zMlQ3PTd4IN88US=> MkLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
HH NHjCZVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3pdXZKSzVyPUOuOFc3PzZizszN NIf4d2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
RO82-W-1 NY\w[INST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTNwNEm4OVUh|ryP NFPJU5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK|5USU6JRWK8M4E,
CCRF-CEM MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHDTWM2OD1|LkWwOFg5KM7:TR?= Mo\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pFGFR2 / FGFR2 ; 

PubMed: 24968263     


PD173074 and MK2461 inhibit FGFR2 phosphorylation. Cells were treated for 1 hour with a titration of PD173074 as described in Materials and methods. Lysates were prepared and 50 ug protein was subjected to SDS-PAGE and western blotting with phospho Y653/654 FGFR and MAB6841 total FGFR2 antibody.

p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1; 

PubMed: 24968263     


Time course of inhibition for multiple signaling proteins. NCI-H716 cells were treated with 100 nM PD173074 for the indicated times and signaling pathways were analyzed by SDS PAGE and western blotting. 100 nM PD173074 was selected because this amount caused full inhibition of pERK at the 2 hour time point. “p” indicates phosphoprotein, and the phosphorylation sites are listed in Methods. Terminology on the right side of figure groups proteins according to the time at which inhibition or protein loss occurs.

24968263
Growth inhibition assay
Cell viability; 

PubMed: 24968263     


B. PD173074 and MK2461 inhibit NCI-H716 cell growth. Cell lines were plated at 4000 cells/well and incubated overnight. NCI-H716 cells were treated with a titration of PD173074 as described in Materials and Methods. Cell growth was measured with Vialight reagent, and growth was presented relative to untreated cells. C. PD173074 and MK2461 selectively inhibit growth of NCI-H716 cells. Colon cancer cell lines listed were plated at 4000 cells/well and 24 hours later were treated with a titration of compounds. 4 days later cell growth was measured with vialight and IC50s were calculated from graph pad prism. 

24968263
体内研究 PD173074在1 mg/kg/day或2 mg/ka/day对小鼠给药可以剂量依赖性的方式有效阻止由FGF或VEGF诱导的血管生成,并没有明显的毒性。[1] PD173074抑制FGFR3突变体转染的NIH 3T3细胞在裸鼠体内生长。在KMS11异种移植瘤模型中,PD173074抑制FGFR3导致肿瘤生长延缓,小鼠的存活率提高。[4] 在H-510异种移植体中,PD173074阻断肿瘤生长和cisplatin相似,与对照假治疗的动物相比增加中位生存期。在H-69异种移植体中,PD173074在50%小鼠中的诱导作用长于6个月。这些效应是和切除肿瘤中增加的细胞凋亡相关的,而非破坏肿瘤血管。[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)

激酶实验:[1]
- 合并

体外激酶抑制试验:

检测是使用全长FGFR-1激酶在100微升含25 mM HEPES缓冲液(pH7.4),150 mM氯化钠,10 mM MnCl2,0.2 mM的原钒酸钠,750 μg/mL谷氨酸和酪氨酸(4:1)的无规共聚物,各种浓度的PD173074,和60至75 ng酶中进行的。该反应通过加入[γ-32P]ATP(含有0.4 μCi of [γ-32P]ATP的5 μM ATP)起始,样品在25°C孵育10分钟。反应通过加入30%三氯乙酸和材料的沉淀到玻璃纤维滤垫上终止。过滤器用15%三氯乙酸洗涤三次,掺入[32P]到谷氨酸酪氨酸聚合物衬底是通过计算保留在过滤器上的放射性来确定,通过WALLAC1250 betaplate阅读器读取。非特异性的活性被定义为温育不含酶的样品保留在过滤器上放射性。特异活性被确定为总活性(酶加缓冲液)减去非特异性活性。PD173074抑制FGFR-1的酶活性的IC50浓度用图解法测定。
细胞实验:[4]
- 合并
  • Cell lines: KMS11和 KMS18
  • Concentrations: 溶解在DMSO中至终浓度~100 nM
  • Incubation Time: 48小时
  • Method: 在aFGF/肝素的存在下,细胞在PD173074浓度梯度中孵育48小时。活细胞的百分比由MTT法检测。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 诱导角膜新生血管的瑞士韦伯斯特小鼠
  • Dosages: 约2 mg/kg/day
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (190.95 mM)
Ethanol 100 mg/mL (190.95 mM)
Water 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+corn oil
15mg/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 523.67
化学式

C28H41N7O3

CAS号 219580-11-7
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:

    What is the half-life of PD173074(S1264) in vivo?

  • 回答:

    According to literature research, PD173074 is given twice daily because it has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID