Afatinib (BIBW2992)

For research use only. Not for use in humans.

目录号:S1011 中文名称:阿法替尼

Afatinib (BIBW2992) Chemical Structure

CAS No. 850140-72-6

Afatinib (BIBW2992) 不可逆地抑制EGFR/ErbB,包括EGFR(wt)EGFR(L858R),EGFR(L858R/T790M),ErbB2(HER2)和ErbB4(HER4),在无细胞试验中IC50分别为0.5 nM,0.4 nM,10 nM,14 nM和1 nM。Afatinib可诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1964.25 现货
RMB 977.68 现货
RMB 4652.69 现货
RMB 10401.3 现货
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客户使用Selleck生产的Afatinib (BIBW2992)发表文献285篇:

产品安全说明书

EGFR抑制剂选择性比较

生物活性

产品描述 Afatinib (BIBW2992) 不可逆地抑制EGFR/ErbB,包括EGFR(wt)EGFR(L858R),EGFR(L858R/T790M),ErbB2(HER2)和ErbB4(HER4),在无细胞试验中IC50分别为0.5 nM,0.4 nM,10 nM,14 nM和1 nM。Afatinib可诱导自噬。
靶点
EGFR (L858R) [1]
(Cell-free assay)
EGFR (wt) [1]
(Cell-free assay)
ErbB4 [2]
(Cell-free assay)
EGFR (L858R/T790M) [1]
(Cell-free assay)
HER2 [1]
(Cell-free assay)
0.4 nM 0.5 nM 1 nM 10 nM 14 nM
体外研究

BIBW2992不可逆地抑制EGFR/HER2,在体外作用于野生型EGFR ,L858R突变型EGFR, L858R/T790M 双突变型EGFR,及HER2时IC50分别为0.5, 0.4, 10, 14 nM。在体外实验中,BIBW2992不管作用于野生型EGFR/HER2还是突变型EGFR/HER2都显示出强大的活力,与gefitinib作用于L858R突变型EGFR的活力差不多,但是要比gefitinib 作用于L858R-T790M双突变型EGFR的活力大100倍。在体外,BIBW2992有效抑制所有实验类型细胞的EGFR/HER磷酸化作用。比如人类扁平上皮癌A431细胞系表达的野生型EGFR, 鼠类NIH-3T3细胞转染的野生型HER2 , 以及乳腺癌BT-474细胞系和胃癌NCI-N87细胞系表达的内源性HER2。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 M4G0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwMEC1O|Ih|ryP M3Lyb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
KASUMI-1 Ml3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwMEC5NVEh|ryP M4HCdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
HCC2218 NYXUNWNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\CWFVKSzVyPUCuNFA6QDdizszN M1nCU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
KARPAS-45 Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jCU2lEPTB;MD6wNVY4OSEQvF2= MljKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
HSC-4 M13YSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwMEG3OFgh|ryP MlnEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
CHL-1 MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXZeJU5UUN3ME2wMlAyQDN7IN88US=> M{Xoc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
KY821 NWe0UohuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLmZZp1UUN3ME2wMlAzODZizszN NEX4d|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
NCI-N87 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPQ[phVUUN3ME2wMlAzPzd|IN88US=> M33lWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
DOK NEHldHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHSOo5ZUUN3ME2wMlA{OTl2IN88US=> M4DOfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
DSH1 NHPoOoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwMEOzNVQh|ryP NUntO|czRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
MDA-MB-175-VII MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfDTo9iUUN3ME2wMlA{PDF4IN88US=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
NCI-H2170 NWPGdXB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\CbpNoUUN3ME2wMlA{PzJ6IN88US=> NHLmcHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
BT-474 MnfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH5e3lKSzVyPUCuNFQ6QDZizszN MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
EFO-27 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTiZYZKSzVyPUCuNFUyQDJizszN MljVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
NCI-H720 M4XDfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInnfnNKSzVyPUCuNFU{OjVizszN M1PqVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
PC-14 NXSwR3k5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwMEW2Olgh|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
EC-GI-10 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMEW5NVIh|ryP M33kelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
KYSE-450 NVHpNJpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP4VJZHUUN3ME2wMlA2QTd6IN88US=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
BPH-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn20TWM2OD1yLkC1PVg5KM7:TR?= MmDHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
NCI-H292 NWjVV5d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1viUWlEPTB;MD6wOlA6KM7:TR?= MmPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
H9 NF;JNGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwMEexN|Ih|ryP MnLsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
NCI-H526 NIHae|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1f1RWlEPTB;MD6wO|gzOyEQvF2= NWLF[IRWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
NCI-H1623 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMEiwNlUh|ryP NEPvcpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
KYSE-140 NUjPWpRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPVNnpKSzVyPUCuNFg{OyEQvF2= NWHVWpVsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
Ca9-22 NWDURlFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;wfWlEPTB;MD6wPFM2OyEQvF2= NGDufIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
AU565 NIHuR2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XUUGlEPTB;MD6wPFUxPCEQvF2= NHvtWJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
ZR-75-30 M2TNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjKTFBKSzVyPUCuNFk2PDVizszN M2PMT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
NCI-H1770 NWTLUIQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHmTWM2OD1yLkGwNlgh|ryP MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
LB2241-RCC NULvO2hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnoeFlpUUN3ME2wMlExQDh2IN88US=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
CAL-39 NVznWndOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMUG3PVIh|ryP MnjVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
UACC-893 NH\CSGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TneWlEPTB;MD6xNVg5PSEQvF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
LU-65 NILldYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC3VIsxUUN3ME2wMlEzPjN|IN88US=> M3uy[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
HN M13jXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMUOwO|ch|ryP M13SN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
TI-73 NYHhXGFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwMUS3NVUh|ryP NYnWR45JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
KU812 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4O3WmlEPTB;MD6xOVQ2PiEQvF2= M3LlfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
SW13 NVvCV|ZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTBwMU[yNVYh|ryP M1LXTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
BB30-HNC NETKUZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMU[1O|Yh|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
HSC-2 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlqyTWM2OD1yLkG2PFM4KM7:TR?= NHzSUWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
BV-173 NX3ndI05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rNcWlEPTB;MD6xO|U6PiEQvF2= M1y2NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
CAL-27 NIDVTFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[5b2VKSzVyPUCuNVc3OzZizszN NF;rTYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
SBC-1 M1fmUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLLOolKSzVyPUCuNVg6PTlizszN NYO5T5drRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CIP2A / p-AKT / AKT / PARP; 

PubMed: 25537503     


Time-dependent effects of afatinib on CIP2A, p-AKT and apoptosis-related proteins in the sensitive H358 and resistant H460 cells. Cells were exposed to 10 μM afatinib for up to 48 hours. Immunoblots were scanned and quantitated to determine the ratio of the level of CIP2A to actin. Data are mean ± SD. n = 3 for the different time intervals.

p-EGFR / p-IGF1R / p-ERK / p-AKT; 

PubMed: 26052929     


Effects of afatinib on EGFR and IGF1R Signaling Pathways. H1975 cells were treated with afatinib with various doses and cell lysates were subjected to Western blot analysis. Afatinib effectively inhibits p-EGFR and p-ERK while p-AKT was partially inhibited. IGF1R phosphorylation was increased upon afatinib treatment in H1975 cells.

p-VEGFR2 / VEGFR2 / JAG1 / DLL4 / NICD1 ; 

PubMed: 28533486     


HUVECs were cultured in the presence of Vatalanib (100 nM) or DBZ (10 nM) for 1 h and then treated for 15 min with rhgal-3 (37 nM) and cultured for additional 6 hrs. After this period, the total protein was isolated and the protein levels of galectin-3, NICD1, DLL4, JAG1, VEGFR2 and VEGFR2-p were assessed by Western blot. β-actin was used as a loading control.

25537503 26052929 28533486
Growth inhibition assay
Cell apoptosis; 

PubMed: 25537503     


Dose-dependent effects of afatinib on apoptosis. Data are mean ± SD. n = 3 for each concentration. *, p < 0.05, **, p < 0.01, vs. no afatinib. 

Cell viability; 

PubMed: 26515464     


A. MTS assay for Ba/F3 cells harboring EGFR exon 19 deletion and L858R. The proportional cell viability is shown. B. MTS assay for Ba/F3 cells harboring EGFR exon 19 deletion+T790M and L858R+T790M. The proportional cell viability is shown. C. MTS assay for Ba/F3 cells harboring wild type EGFR. The proportional cell viability is shown. Erlotinib, afatinib, osimertinib, and rociletinib were used as EGFR-TKIs. Error bars indicate standard deviation.

25537503 26515464
Immunofluorescence
p65; 

PubMed: 26317651     


Effects of different treatments on the nuclear translocation of the NF-κB subunit p65. A2780T cells were treated with 2.5 μM afatinib for 48 hours, or 10 μM PDTC for 2 hours. Subsequently, the NF-κB subunit p65 (red) was localized by immunofluorescence and a confocal microscopy. Nuclei were stained with DAPI (blue). Scale bar = 10 μM.

vacuoles; 

PubMed: 29713246     


Autophagy activation upon treatment with Afatinib and Sorafenib was validated using immunofluorescence in order to visualize a creation of autophagosomes; ×60 magnification. DMSO treatment was used as control. Green—autophagy vacuoles; Blue—Hoechst, nuclear staining. 

26317651 29713246
体内研究 活体研究时按实验对象体重,每千克口服20 mg BIBW2992持续25天,肿瘤产生明显的衰退现象,通过肿瘤切片的免疫组织化学染色观察发现,EGFR和AKT的磷酸化作用收到抑制。因此,正如lapatinib和neratinib, BIBW2992是次代酪氨酸激酶抑制剂,不可逆地抑制人类EGFR2(HER2)和EGFR激酶。BIBW2992不仅能和原代酪氨酸激酶如erlotinib和gefitinib一样有效抑制EGFR突变型,而且还能作用于抗erlotinib和gefitinib的EGFR。[1]

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

体外激酶活性实验:

人类EGFR和L858R/T790M双重突变型EGFR 的酪氨酸激酶区域与谷胱甘肽巯基转移酶区域相接,提取酪氨酸激酶区域的方法见补充说明。在有和没有BIBW2992时分别测定酶活。使用杆状病毒系统克隆HER2激酶,用类似提取EGFR激酶域的方法提取HER2激酶域。
细胞实验:

[1]

- 合并
  • Cell lines: NSCLC细胞
  • Concentrations: 0-10 μM
  • Incubation Time: 1小时
  • Method:

    细胞按1×104密度转移到96孔板上,在无血清培养基上过夜培养,用于EGFR磷酸化实验。第二天添加包含BIBW2992的混合物,培养基在37oC温育1小时。在室温下用100 ng/ml EGF刺激10分钟。细胞用冰冻PBS冲洗,然后每孔用120 μl HEPEX buffer萃取,然后在室温下震荡1小时。每孔中所有2×104细胞都用于HER2磷酸化实验。在涂有链霉亲和素的板上加用封闭液按1:100比例稀释的抗EGFR的生物素和c-erb2/HER2肿瘤蛋白Ab-5-生物素。上述步骤得到的萃取物转移到有抗体包被的孔中,室温下温育1小时。彩色显影的测法见补充说明,吸光度为450纳米。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 雌性无胸腺NMRI-nu/nu鼠
  • Dosages: 20 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 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):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/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 485.94
化学式

C24H25ClFN5O3

CAS号 850140-72-6
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、SDS / 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、SDS / 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

临床试验信息