Gefitinib (ZD1839)

目录号:S1025 别名: Iressa 中文名称:吉非替尼

仅限科研使用

Gefitinib (ZD1839)是一种EGFR抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。

Gefitinib (ZD1839) Chemical Structure

CAS: 184475-35-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1574.78 现货
RMB 1227.69 现货
RMB 2205.98 现货
大包装 有超大折扣
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客户使用Selleck生产的Gefitinib (ZD1839)发表文献586篇:

产品安全说明书

EGFR抑制剂选择性比较

相关EGFR产品

生物活性

产品描述 Gefitinib (ZD1839)是一种EGFR抑制剂,作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。
特性 Gefitinib是有效的EGFR酪氨酸激酶抑制剂。
靶点
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
体外研究

Gefitinib 作用于高和低表达EGFR的细胞系,包括NR6, NR6M 和 NR6W 细胞系,有效抑制EGFR上全部酪氨酸磷酸化位点。磷酸化位点 Tyr1173和Tyr992敏感性较低,需要高浓度Gefitinib才能抑制。Gefitinib作用于NR6W细胞,高效阻断PLC-γ磷酸化, IC50为27nM。NR6wtEGFR 和NR6M细胞系具有低水平PLC-γ磷酸化, IC50 分别为 43 nM和 369 nM。Gefitinib抑制AKT磷酸化,作用于低EGFR和EGFRvIII表达的细胞系, IC50 分别为220 和263nM。Gefitinib按 0.1 到 0.5μM剂量处理,显著促进而不是废除 NR6M细胞形成集落。然而, 2μM Gefitinib 完全抑制 NR6M 集落形成。Gefitinib 作用于高和低EGFR表达的细胞系,EGF 刺激72小时后,快速抑制EGFR 和ERK 磷酸化,这种作用存在剂量依赖性。[1]Gefitinib抑制 EGF驱动的未转化MCF10A 细胞生长,IC50为 20 nM。[2] Gefitinib 作用于MDA-MB-231细胞,抑制EGF信号。Gefitinib严重抑制细胞数的增多,这种作用存在剂量依赖性。 [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1975 NYLqUoY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTJzLkS2NUDPxE1? MnrMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HT MkCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHRbnNKSzVyPUKxMlQ{OzFizszN NX7y[2VoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HUTU-80 MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzXTWM2OD1{MT60N|M3KM7:TR?= M13O[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
PA-1 NVvZOolkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTtTWM2OD1{MT6yO|g4KM7:TR?= MkTlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HOP-62 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGyNI5QUUN3ME2yNU4zPzh2IN88US=> NF7ZcYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
GI-1 NInocZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTJzLkG3JO69VQ>? M3T3WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MC116 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nCemlEPTB;MkGuNFczOyEQvF2= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
A375 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrpcJZWUUN3ME2yNU4xPTZ5IN88US=> M1nzbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
IST-SL1 Mk\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnGwTWM2OD1{MD63PFc6KM7:TR?= M{HLXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
TE-5 NHOydY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHYSZM2UUN3ME2yNE44PDh{IN88US=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
SiHa NFHDOo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnvTWM2OD1{MD6zO|EzKM7:TR?= NVn0WIo2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
LB2518-MEL NF\ON4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHwWlBpUUN3ME2yNE4{PzN7IN88US=> M3nORlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
BB49-HNC NYOwRlg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn76TWM2OD1zOT65NkDPxE1? NI\yVIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HGC-27 Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHEbHdKSzVyPUKwMlE{QTRizszN NWrUXFdKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
Becker MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrwSGVKSzVyPUG5Mlg2PDdizszN M3HGVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
TYK-nu M3rieGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHJTWM2OD1zOT64N|c5KM7:TR?= NEnuXXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H650 NEXGZ4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3Le4ZKSzVyPUG5Mlc2ODhizszN NIDDZ449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
WM-115 NFXQTJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLi[o9YUUN3ME2xPU43Pzd2IN88US=> M1jZfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HuH-7 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPlVodKSzVyPUG5Mlc1OjFizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-N87 NW\IPJRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF7LkW5PVIh|ryP NGX3S5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H1048 MoXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULKUXVGUUN3ME2xPU4zOzJ4IN88US=> NXn3WFFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H446 M3S4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDBTWM2OD1zOT6zOVg6KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1437 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHHTWM2OD1zOT6wOFY4KM7:TR?= MnL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
D-263MG NIDieFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfqcIp3UUN3ME2xPU4xOTd{IN88US=> NH;BSGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
MFH-ino NUT1b4s2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HyR2lEPTB;MUiuPVY3QSEQvF2= MnvsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
U-266 NVXtSFkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LUfWlEPTB;MUiuPFY1QSEQvF2= M4DW[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
OVCAR-8 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXqTWM2OD1zOD65Nlc3KM7:TR?= MmmzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
KNS-42 MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC3TWM2OD1zOD64NFE2KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
U251 NH73VoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK3emhKSzVyPUG4Mlc{PDdizszN M1HEblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
MFE-280 NHj1WGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jIXGlEPTB;MUiuO|I6OyEQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H1563 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLqTWM2OD1zOD63NVI1KM7:TR?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
MDA-MB-361 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLLU4Z[UUN3ME2xPE42PTh6IN88US=> MkjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HLE NV\ucHpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUmxZlZYUUN3ME2xPE4{OTR6IN88US=> MlfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
SW982 NVjFW|NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorjTWM2OD1zOD60NFc2KM7:TR?= M4f4Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
KM-H2 NVf6S4V2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXuVZVEUUN3ME2xO{46PDFzIN88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
D-502MG NV7ZWoFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vIc2lEPTB;MUeuPVgxQCEQvF2= MmjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
ES8 NWrqcmhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrB[pZLUUN3ME2xO{45PTl|IN88US=> NELYWpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
SF268 MlXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nYSmlEPTB;MUeuOlk3QSEQvF2= NFe0WY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
Calu-6 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF5Lk[3PFIh|ryP NUPLeXlTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SW1783 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfSTWM2OD1zNz62OFE2KM7:TR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
NCI-H747 NY\iU|E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTF5LkWyPVch|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N|kwLz6VQV7HSXI9N2F-
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Assay
Methods Test Index PMID
Western blot phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT Cyclin D1/ p16 / p27 / pRb uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP PPAR-γ 22586683 18559346 23102728 23409107
Immunofluorescence EGFR / LC3 PPAR-γ p-EGFR / β-catenin 31196210 23409107 23461856
Growth inhibition assay GI50 23409107
体内研究

Gefitinib 作用于无胸腺裸鼠,抑制SKOV3 或MDA-MB-231 肿瘤生长。Gefitinib高效作用于两种类型肿瘤。处理14天后,MDA-MB-231肿瘤和SKOV3肿瘤生长抑制分别为71%和32%。

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)

细胞实验:

[1]

  • Cell lines: NR6, NR6M 和 NR6W 细胞
  • Concentrations: 0 μM -2 μM
  • Incubation Time: 72 小时
  • Method:

    呈指数生长的细胞,包括 NR6, NR6M, NR6M和NR6W细胞按6倍接种在96孔板上,每孔为2000个细胞, 粘附,随后在PBS 中清洗,然后在含0.5% FCS的培养基上温育过夜。使用不同浓度(0-2 μM) Gefitinib或溶质对照DMSO 和EGF 处理细胞。诱导NR6wtEGFR和NR6W 细胞增殖的EGF最佳浓度已经测定,因此NR6wtEGFR和 NR6W 细胞中分别加入10 nM和 0.1 nM EGF。NR6 和NR6M细胞中不加入EGF。72 小时后,通过MTT 增殖检测测量细胞数。

动物实验:

[6]

  • Animal Models: 携带 SKOV3或MDA-MB-231肿瘤的无胸腺裸鼠
  • Dosages: 75 mg/kg
  • Administration: 饲喂处理

溶解度(25°C)

体外

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):
1% CMC Na

30mg/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 446.90
化学式

C22H24ClFN4O3

CAS号 184475-35-2
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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

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,: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: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: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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03292133 Recruiting Drug: EGF816|Drug: Gefitinib Lung Cancer Massachusetts General Hospital|Novartis October 31 2017 Phase 2
NCT03122717 Active not recruiting Drug: Gefitinib|Drug: Osimertinib Non-Small Cell Lung Cancer Dana-Farber Cancer Institute|AstraZeneca May 9 2017 Phase 1|Phase 2
NCT02932345 Completed -- EGFR Mutation Positive Advanced Non-small-cell Lung Cancer AstraZeneca October 31 2016 --
NCT02824458 Recruiting Drug: Apatinib|Drug: Gefitinib|Drug: Placebo EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors Sun Yat-sen University June 2016 Phase 3
NCT02804100 Unknown status -- Carcinoma Non-Small-Cell Lung|Bronchial Neoplasms|Carcinoma Bronchogenic|Lung Diseases|Lung Neoplasms Wenzhou Medical University May 2016 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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操作手册

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常见问题及建议解决方法

问题 1:
I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?

回答:
S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.