Afatinib (BIBW2992)

For research use only. Not for use in humans.

製品コードS1011

Afatinib (BIBW2992)化学構造

CAS No. 850140-72-6

Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 41800
JPY 21900
JPY 36800
JPY 96600
JPY 212800
JPY 361600
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バルク問合せ

文献中Selleckの製品使用例(268)

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
ターゲット
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
体外試験

BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatinib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 NFq4[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMEC1O|Ih|ryP M{jaR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
KASUMI-1 NWHRelN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X6OmlEPTB;MD6wNFkyOSEQvF2= M1z0T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
HCC2218 M3P2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LnOWlEPTB;MD6wNFk5PyEQvF2= NGe1V4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
KARPAS-45 MlntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3PTWM2OD1yLkCxOlcyKM7:TR?= M3q2RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
HSC-4 MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\wZWNKSzVyPUCuNFE4PDhizszN NF;pVYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
CHL-1 M1\mTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHJTWM2OD1yLkCxPFM6KM7:TR?= MnTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
KY821 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTG[IE2UUN3ME2wMlAzODZizszN M4TMV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
NCI-N87 MkK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljtTWM2OD1yLkCyO|c{KM7:TR?= MlfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
DOK NVvTTJpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1juR2lEPTB;MD6wN|E6PCEQvF2= NGnFbGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
DSH1 NXvSeINoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPKTWM2OD1yLkCzN|E1KM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
MDA-MB-175-VII MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3SOFVHUUN3ME2wMlA{PDF4IN88US=> NYrHbZVDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
NCI-H2170 M3;zU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnftTWM2OD1yLkCzO|I5KM7:TR?= NHXrN5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
BT-474 M{\V[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnKTWM2OD1yLkC0PVg3KM7:TR?= NUTkcnBIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
EFO-27 M2PQ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnmzTWM2OD1yLkC1NVgzKM7:TR?= NIHBPXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
NCI-H720 NIXXcI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;LcVlKSzVyPUCuNFU{OjVizszN NXex[4xMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
PC-14 NYnjZmtrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;mW4NSUUN3ME2wMlA2PjZ6IN88US=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
EC-GI-10 M3rFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwMEW5NVIh|ryP Ml2xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
KYSE-450 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWyTWM2OD1yLkC1PVc5KM7:TR?= NIW3PIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
BPH-1 NFnhcmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nje2lEPTB;MD6wOVk5QCEQvF2= M1fq[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
NCI-H292 NIPocnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jXUmlEPTB;MD6wOlA6KM7:TR?= NYDne3NHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
H9 NV\RWoU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnMR3J5UUN3ME2wMlA4OTN{IN88US=> NGP0[pQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
NCI-H526 NHHXd2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDnTWM2OD1yLkC3PFI{KM7:TR?= M1jIPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
NCI-H1623 MnvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ixXmlEPTB;MD6wPFAzPSEQvF2= NETRd4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
KYSE-140 NELETmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXiyVI52UUN3ME2wMlA5OzNizszN MlewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
Ca9-22 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\ETWM2OD1yLkC4N|U{KM7:TR?= NVLxW5IyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
AU565 M4m0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LqO2lEPTB;MD6wPFUxPCEQvF2= NXrDZ5hqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
ZR-75-30 MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXMXVhKSzVyPUCuNFk2PDVizszN M4S5ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
NCI-H1770 NXrxUnFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEi3b4xKSzVyPUCuNVAzQCEQvF2= MnThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
LB2241-RCC M1fuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3RT4Q4UUN3ME2wMlExQDh2IN88US=> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
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UACC-893 NVjJSld3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H5[WlEPTB;MD6xNVg5PSEQvF2= NFrk[Zo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
LU-65 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV76ZWVCUUN3ME2wMlEzPjN|IN88US=> NFvpXHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTd|NkW1M{c,W0GQR1XSQE9iRg>?
HN NVrGOGY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:zTWM2OD1yLkGzNFc4KM7:TR?= NWHRXIRPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5M{[1OU8oRlODTlfFVlww[T5?
TI-73 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLnPGduUUN3ME2wMlE1PzF3IN88US=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
KU812 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmryTWM2OD1yLkG1OFU3KM7:TR?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
SW13 M32zUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwMU[yNVYh|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
BB30-HNC NVfwNlRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXJeYlKSzVyPUCuNVY2PzZizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
HSC-2 MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3XTJRKSzVyPUCuNVY5OzdizszN MoX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
BV-173 NYT2OmtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDKTWM2OD1yLkG3OVk3KM7:TR?= MnPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
CAL-27 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLs[pZKSzVyPUCuNVc3OzZizszN MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
SBC-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1qx[GlEPTB;MD6xPFk2QSEQvF2= M4XScFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzN4NUWvK|5USU6JRWK8M4E,
CAL-33 NYD1NoluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nvdWlEPTB;MD6yNFE5PCEQvF2= MlXlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OzZ3NT:nQnNCVkeHUkyvZV4>
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MC-IXC NIG5[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HwUGlEPTB;MUGuOlczQCEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVc{PjV3Lze+V2FPT0WUPD;hQi=>
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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
体内試験 Daily oral administration of BIBW2992 at 20 mg/kg for 25 days results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Reduced phosphorylation of EGFR and AKT is confirmed by immunohistochemical staining of tissue sections. Therefore, like lapatinib and neratinib, BIBW2992 is a next generation tyrosine kinase inhibitor (TKI) that inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases irreversibly. BIBW2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those insensitive to these standard therapies. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

In vitro kinase activity assays:

The wild type tyrosine kinase domain of the human EGFR as well as that of the EGFR L858R/T790M double mutant are fused to Glutathione-S-transferase (GST), and extracted. Enzyme activity is then assayed in the presence of the inhibitor BIBW2992, serially diluted in 50% DMSO. A random polymer pEY (4:1) is used as substrate and biotinylated pEY (bio-pEY) is added as a tracer substrate. The kinase domain of HER2 is cloned using the baculovirus system and extracted similarly to that of EGFR kinase. Details of assays for EGFR, HER2, SRC, BIRK and VEGFR2 kinase activity are available in Supplementary information.
細胞試験:

[1]

- 合併
  • 細胞株: NSCLC cells
  • 濃度: 0-10 μM
  • 反応時間: 1 hour
  • 実験の流れ:

    1 × 104 NSCLC cells are transferred into each well of a 96-well plate and cultured overnight in serum-free media for the EGFR phosphorylation assay. After addition of BIBW2992 on the next day, the plates are incubated at 37 °C for 1 hour. EGF-stimulation is done using 100 ng/mL for 10 min at room temperature. Cells are washed with ice cold PBS, extracted with 120 μL HEPEX buffer per well and shaken at room temperature for 1 hour. In all 2 × 104 cells per well is used for the HER2 phosphorylation assay. Streptavidin precoated plates are coated with anti-EGFR-biotin at 1:100 dilution in blocking buffer and c-erb2/HER2 oncoprotein Ab-5(Clone N24)-Biotin. Cell extracts is then transferred to the antibody-coated wells and incubated at room temperature for 1 hour. Extinction is measured at 450 nm.


    (参考用のみ)
動物試験:

[1]

- 合併
  • 動物モデル: Athymic NMRI-nu/nu female mice
  • 投薬量: 20 mg/kg
  • 投与方法: Oral administration
    (参考用のみ)

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 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 485.94
化学式

C24H25ClFN5O3

CAS No. 850140-72-6
Storage powder
in solvent
別名 N/A
Smiles CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04497584 Not yet recruiting Drug: Afatinib + Prednisone Advanced Squamous Non Small Cell Lung Cancer University of Texas Southwestern Medical Center March 1 2021 Phase 2
NCT04413201 Recruiting Drug: Afatinib|Drug: Osimertinib Non-squamous NSCLC Michael Hopp|Boehringer Ingelheim|Johannes Gutenberg University Mainz September 11 2020 Phase 4
NCT04206787 Recruiting Drug: Afatinib Non-squamous Non-Small Cell Lung Cancer Boehringer Ingelheim May 20 2020 --
NCT04158947 Recruiting Drug: Afatinib|Drug: T-DM1 HER2-positive Breast Cancer|Brain Metastases xuexin he|Second Affiliated Hospital School of Medicine Zhejiang University May 10 2020 Phase 2
NCT03711422 Unknown status Drug: Afatinib Non-small Cell Lung Cancer|Leptomeningeal Disease|Central Nervous System Metastases National Cancer Centre Singapore October 2018 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What’s the recommendation about reconstitution of the compound for in vivo animal study?

  • 回答:

    For in vivo experiment of afatinib, we recommend 0.5% methylcellulose/0.2% Tween 80 as vehicle.

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