Erlotinib (OSI-774)

製品コード:S7786 別名:CP358774, NSC 718781, Tarceva

For research use only.

Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.

Erlotinib (OSI-774)化学構造

CAS No. 183321-74-6

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 15900
JPY 18100
JPY 34700

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(520)

製品安全説明書

EGFR阻害剤の選択性比較

相関EGFR製品

生物活性

製品説明 Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
ターゲット
EGFR [1]
(Cell-free assay)
2 nM
体外試験

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon cancer cells. [1] Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. [2] Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [3] The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. [4] Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [5]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SKBR3 cells MVjGeY5kfGmxbjDhd5NigQ>? Mkj1TY5pcWKrdHnvckBw\iCKRWKyJIlvKGi3bXHuJHNMSlJ|IHPlcIx{KGK7IFjUVmYh[XO|YYmsJGlEPTB;MT64PUDPxE1w NYLodlRRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4NVU1OTJpPkG5PFE2PDF{PD;hQi=>
human A431 cells NIDsTI5HfW6ldHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKEWJRmKgbY4hcHWvYX6gRVQ{OSClZXzsd{BjgSCKVGLGJIF{e2G7LDDJR|UxRTBwNEKg{txONg>? NFjoe4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUixOVQyOid-MUm4NVU1OTJ:L3G+
Huh7.5 NXLpWnI5SW62aY\pdoFtKGG|c3H5 NF\RZ5A{OCCvaX7z MmLERY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGMhfmm{dYOgTlYwUk[KIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFcvPSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGhEXiC{ZYDsbYNifGmxbjDwdoV1emWjdHXkJIZweiB|MDDtbY5{KG[xbHzve4VlKGK7IHnu[oVkfGmxbjDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliYXzhcYFzKGKudXWg[JlmKGKjc3XkJIZtfW:{ZYPj[Y5k\SCjc4PhfS=> MkP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7MkWyNFgoRjJ4OUK1NlA5RC:jPh?=
Huh7.5 MkP0RY51cX[rcnHsJIF{e2G7 Mn;0O|IhcHK| NX;FZpJSSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KENidnnyeZMhUjZxSl\IJIlv\mWldHXkJIlvKGi3bXHuJGh2cDdwNTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vKG2nYYP1doVlKGGodHXyJFczKGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVAhRSByLkWg{txONg>? NF36PVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiyNlc{QSd-MkW4NlI4Ozl:L3G+
Huh7.5 MlfQRY51cX[rcnHsJIF{e2G7 MWK3NkBpenN? M3vkZ2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJGo3N0qISDDlcIVkfHKxcH;yZZRm\CCrbjDoeY1idiCKdXi3MlUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDpcpRz[WOnbHz1cIFzKGmwZnXjeIl3cXS7IHTyeYchfHKnYYTl[EBmfmW{eTCyOEBpenNiZn;yJFczKGi{czDt[YF{fXKnZDC3NkBpenNicH;zeEBmdGWldILvdI9z[XSrb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD61JO69VS5? MoXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MkK3N|koRjJ3OEKyO|M6RC:jPh?=
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A431 NIjGUnNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUnEUYJXPzJiaILz MkXmS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gRVQ{OSClZXzsd{BwfmW{ZYjwdoV{e2mwZzDFS2ZTKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUCgQUAxNjR5IN88UU4> M37FSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUizO|Q2Lz5zN{m4N|c1PTxxYU6=
A431 M3;QPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkDzO|IhcHK| NGP3XHFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUCgQUAxNjlzNTFOwG0v M1i4U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OU[5OFY2Lz5zOUm2PVQ3PTxxYU6=
BA/F3 M2fEcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn:3PVYhcHK| Ml3jS5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCHR1\SJGRmdDFibYX0ZY51KGGodHXyJFk3KGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiR1m1NEA:KDBwNTFOwG0v MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODJ{MkezN{c,OjB{MkK3N|M9N2F-
BA/F3 MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnGPVYhcHK| M3jGTGdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiRVfGVkBF\Wx|IH31eIFvfCCjZoTldkA6PiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFfJOVAhRSByLkWg{txONg>? MlnsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB{MkK3N|MoRjJyMkKyO|M{RC:jPh?=
BA/F3 MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NITCWpg6PiCqcoO= M{LMXmdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiRVfGVkBF\Wx3IH31eIFvfCCjZoTldkA6PiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFfJOVAhRSByLkWg{txONg>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODJ{MkezN{c,OjB{MkK3N|M9N2F-
BA/F3 NV\IZ3U1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHPtbY86PiCqcoO= M4robGdzd3e2aDDpcohq[mm2aX;uJI9nKG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiRVfGVkBNQDV6UjDteZRidnRiYX\0[ZIhQTZiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDHTVUxKD1iMD61JO69VS5? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODJ{MkezN{c,OjB{MkK3N|M9N2F-
WM266.4 NXvOZnlIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1G3blI1KGi{cx?= MkjBS5Jwf3SqIHnubIljcXSrb36gbY4hcHWvYX6gW20zPjZwNDDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIILl[JVkfGmxbjDhd5NigSxiR1m1NEA:KDhwMUKg{txONg>? NWrUZok4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5PFU6PjJpPkKyPVg2QTZ{PD;hQi=>
A549 MkTnRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2DHVVI1KGi{cx?= M{jR[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7LDDHTVUxKD1iMD6wN{DPxE1w M2\DW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{mxN|Y1Lz5{M{O5NVM3PDxxYU6=
MCF7 NVLRc2xDSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NIDuS48zPCCqcoO= MortRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCPVGSgZZN{[XluIFfJOVAhRSByLkC4JO69VS5? NF2zXYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5NVM3PCd-MkOzPVE{PjR:L3G+
WM266.4 MmXGRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGPqb4gzPCCqcoO= M1P2PWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV12yOlYvPCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBIUTVyIE2gPE4yPCEQvF2u Mnr4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd{M{i4OFEoRjJ5MkO4PFQyRC:jPh?=
NIH3T3 MmnISpVv[3Srb36gZZN{[Xl? MkfwTY5pcWKrdHnvckBw\iCHR1[gd5RqdXWuYYTl[EBpfW2jbjDldoJDOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJG5KUDOWMzDj[YxteyxiSVO1NEA:KDBwMEG5N{DPxE1w NX\tTYhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0PFAzQDRpPkG2OFgxOjh2PD;hQi=>
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erythroleukemia cells NEGz[VRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\zOFkzPCCqcoO= NFfsTVJIem:5dHigbY5pcWKrdHnvckBw\iCvb4Xz[UBmenm2aILvcIV2c2WvaXGgZ4VtdHNiYX\0[ZIhOjRiaILzMEBKSzVyIE2gNkDPxE1w MlfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdzN{i3NlIoRjF5MUe4O|IzRC:jPh?=
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hematopoietic progenitor cells NGnXPGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3qzRmdzd3e2aDDpcohq[mm2aX;uJI9nKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5NqdmdiaHXtZZRweG:rZYTpZ{Bxem:pZX7peI9zKGOnbHzzJIl{d2yjdHXkJIZzd21icH;sfYN6fGinbXnhJJZmemFicHH0bYVvfCCkeTDjc4xwdnliZn;ycYlv\yCjc4PhfUwhUUN3MDC9JFUh|ryPLh?= NIPV[Wo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{G3PFczOid-MUexO|g4OjJ:L3G+
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LoVo NFq0OnpHfW6ldHnvckBie3OjeR?= NIPENZozKGi{cx?= MXPJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHR1\SJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDMc3ZwKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OCB;IECuNFc4KM7:TT6= MnL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{C5PVQoRjJ|OUOwPVk1RC:jPh?=
NCI-H1975 M{W1[GZ2dmO2aX;uJIF{e2G7 MXKyJIhzew>? M2DqZWlvcGmkaYTpc44hd2ZiRVfGVkBNQDV6Uj;UPVcxVSCmb4XicIUhdXW2YX70JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwJF0hPy54IN88UU4> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|MEm5OEc,OjN7M{C5PVQ9N2F-
Sf9 MoL5SpVv[3Srb36gZZN{[Xl? MnXlNVAhdWmwcx?= NFnuN2ZKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JGVITlJia3nuZZNmKGO7dH;wcIF{dWmlIHTvcYFqdiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{BmgHC{ZYPzbY9vKH[nY4Tvdk1qdm[nY4Tl[EBqdnOnY4Sgd4Y6KGOnbHzzJIF{e2W|c3XkJIF{KGyndnXsJI9nKGG3dH;wbI9{eGixconsZZRqd25iYX\0[ZIhOTBibXnud{BjgSCGRVzGTWEwfGmvZT3y[ZNwdH[nZDDmcJVwem:vZYTyfUwhUUN3MDC9JFAvODNizszNMi=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Mk[2NEc,OjN7NkK2OlA9N2F-
HepG2 MWLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{LrcVQ5KGi{cx?= MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkGyJO69VS5? MoL3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NkK2OlAoRjJ|OU[yOlYxRC:jPh?=
A549 M4PNPWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MX60PEBpenN? MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMUOg{txONg>? M{jJ[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[yOlYxLz5{M{m2NlY3ODxxYU6=
Sf9 M2fMN2Z2dmO2aX;uJIF{e2G7 MVSxNEBucW6| MUPJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IFXHSnIh[3m2b4DsZZNucWNiZH;tZYlvKCh4NEWgeI8hOTF6NjmgLJVvc26xd36gc5Jq\2mwKTDheZRweGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDpcpNm[3RiU3[5JINmdGy|IIDy[Ylv[3WkYYTl[EBnd3JiMUCgcYlveyCob3zsc5dm\CCkeTDBWHAuVWeFbEKgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiMTDodkBjgSCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTBiPTCwMlA{OiEQvF2u NWfvdXlORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOFQ5PTRpPkK0NVQ1QDV2PD;hQi=>
HepG2 Mof3R5l1d3SxeHnjbZR6KGG|c3H5 MoHuOFghcHK| M2PkS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkGyJO69VS5? MkW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNES4OVQoRjJ2MUS0PFU1RC:jPh?=
A549 M2O2dmN6fG:2b4jpZ4l1gSCjc4PhfS=> MWe0PEBpenN? NWS4dmt1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6xN{DPxE1w M3rZRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUS0PFU1Lz5{NEG0OFg2PDxxYU6=
A431 NUToTIUySW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MlHIO|IhcHK| MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2M{GgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwNEC5JO69VS5? NW\1cItHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxPFM4PDJpPkK0NVg{PzR{PD;hQi=>
NCI-H1975 MVTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoCzO|IhcHK| NEL3[|NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOTl5NTDj[YxteyCneIDy[ZN{cW6pIFXHSnIhXDd7MF2gcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB4Lkmg{txONg>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF6M{e0Nkc,OjRzOEO3OFI9N2F-
KB MlnwSpVv[3Srb36gZZN{[Xl? NILZXosyKGi{ MXjJcohq[mm2aX;uJI9nKEWJRj3zeIlufWyjdHXkJIF2fG:yaH;zdIhwenmuYYTpc44hd2ZiRVfGVkBqdiCqdX3hckBMSiClZXzsd{BqdmO3YnH0[YQh\m:{IEGgbJIheHKrb4KgeI8hTUeIIHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB4IH3pcpMh[nliRVzJV2EtKEmFNUCgQUAxNjBzOTFOwG0v M4j6N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEGxNVI{Lz5{NESxNVEzOzxxYU6=
A431 MofsR5l1d3SxeHnjbZR6KGG|c3H5 NVH3O4J6PzJiaILz NEjjT41EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGW6cILld5NqdmdiRVfGVkBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE44PSEQvF2u MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzMUGyN{c,OjR2MUGxNlM9N2F-
Calu3 M3PVdmN6fG:2b4jpZ4l1gSCjc4PhfS=> NETIO5I4OiCqcoO= NHTuc5lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBE[Wy3MzDj[YxteyCneIDy[ZN{cW6pIFjFVlIh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvQTNizszNMi=> M4X5VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEGxNVI{Lz5{NESxNVEzOzxxYU6=
NCI-H1975 Mkn1R5l1d3SxeHnjbZR6KGG|c3H5 M2i0[VczKGi{cx?= MlrER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHX4dJJme3OrbnegSWdHWiCOOEW4Vk9VPzlyTTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDVwNUGg{txONg>? NGqxfXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxNVEzOyd-MkS0NVEyOjN:L3G+
A431 Mn\tRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M1GzVFczKGi{cx?= Mn3jRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNEOxJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlU3KM7:TT6= Mk\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NkW5OlkoRjJ2NU[1PVY6RC:jPh?=
NCI-H1975 MojSRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmPsO|IhcHK| MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHfl[ol1cW6rYj3y[ZNqe3SjboSgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB5LkC2JO69VS5? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4NUm2PUc,OjR3NkW5Olk9N2F-
Sf9 MnjySpVv[3Srb36gZZN{[Xl? NWPKeXVpOSCqch?= MmTwTY5pcWKrdHnvckBw\iCjdYTvdIhwe3Cqb4L5cIF1cW:wIH;mJJJm[2:vYnnuZY51KEWJRmKgZ5l1d3CuYYPtbYMh\G:vYXnuJEg3PDVidH:gNVE5PiliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIFnfGW{IEGgbJIh[nliRFXMSmlCN3SrbXWtdoV{d2y4ZXSg[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwJF0hOC5yM{Kg{txONg>? MoD6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MEe5PVgoRjJ2NkC3PVk5RC:jPh?=
HepG2 MmTrRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXXDbGtvPDhiaILz MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkGyJO69VS5? NH7UU2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[wO|k6QCd-MkS2NFc6QTh:L3G+
A549 M3Hh[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVu0PEBpenN? MnvwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkGzJO69VS5? M{\TSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkC3PVk5Lz5{NE[wO|k6QDxxYU6=
Sf9 MYrGeY5kfGmxbjDhd5NigQ>? M1;FN|EhcHJ? M4fwbGlvcGmkaYTpc44hd2ZiYYX0c5Bpd3OyaH;yfYxifGmxbjDv[kBGT0[UIHP5eI9xdGG|bXnjJIRwdWGrbjCoZY1qdm9iYXPp[JMhPjR3IITvJFEyQDZrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bi\nSncjCxJIhzKGK7IITpcYUuemW|b3z2[YQh\my3b4LvcYV1enluIFnDOVAhRSByLkCzNkDPxE1w MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ|MESxNkc,OjR4M{C0NVI9N2F-
HepG2 M4[0SmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NG\SRpQ1QCCqcoO= MoK4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6xNkDPxE1w NHXTT|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[zNFQyOid-MkS2N|A1OTJ:L3G+
A549 NHnzbFBCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4TpZlQ5KGi{cx?= NGTLRohCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNVMh|ryPLh?= NF\KbJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[zNFQyOid-MkS2N|A1OTJ:L3G+
Sf9 NV7HTI9VTnWwY4Tpc44h[XO|YYm= NU\JdWFTOSCqch?= M2DhcGlvcGmkaYTpc44hd2ZiYYX0c5Bpd3OyaH;yfYxifGmxbjDv[kBpfW2jbjDISXIzKGO7dH;wcIF{dWmlIHTvcYFqdiBqYX3pco8h[WOrZIOgOlc3KHSxIEGyOFUqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDh[pRmeiBzIHjyJIJ6KHSrbXWtdoV{d2y4ZXSg[ox2d3KxbXX0dpktKEmFNUCgQUAxNjF4IN88UU4> M1iydFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkOwOFEzLz5{NE[zNFQyOjxxYU6=
A431 M{SzWWZ2dmO2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKEWJRmKgbY4hcHWvYX6gRVQ{OSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVAhRSByLkCwNVIh|ryPLh?= M2LWeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEmwOlUzLz5{NEi5NFY2OjxxYU6=
MCF7 NFnHT29EgXSxdH;4bYNqfHliYYPzZZk> NHnBfVZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBGWi2yb4PpeIl3\SCPQ1[3JINmdGy|LDDJR|UxKD1iMD6wNFEzKM7:TT6= Ml6xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
U251 MVXGeY5kfGmxbjDhd5NigQ>? NYmwUItKUW6qaXLpeIlwdiCxZjDWSWdHWjJiaX6gbJVu[W5iVUK1NUBk\WyuczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiYYPzZZktKEmFNUCgQUAxNjF{NEeg{txONg>? M3fkZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEmwOlUzLz5{NEi5NFY2OjxxYU6=
MDA-MB-468 MUjDfZRwfG:6aXPpeJkh[XO|YYm= MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjD0dolxdGVibnXnZZRqfmViTVTBMW1DNTR4ODDj[YxteyxiSVO1NEA:KDBwMkO1NkDPxE1w M2D6[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEmwOlUzLz5{NEi5NFY2OjxxYU6=
MDA-MB-231 NVSxSmxPS3m2b4TvfIlkcXS7IHHzd4F6 NVvJSVBjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hfHKrcHzlJI5m\2G2aY\lJG1FSS2PQj2yN|Eh[2WubIOsJGlEPTBiPTCwMlQ{QDVizszNMi=> NVzkZYk3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PVA3PTJpPkK0PFkxPjV{PD;hQi=>
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MDA-MB-231 NH\ncJlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnmwO|IhcHK| NEHIVJhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOzBwMUKg{txONg>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl{M{O4N{c,Ojh7MkOzPFM9N2F-
MDA-MB-231 MUPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MnTrOFghcHK| NYq0N25{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHnuZ5Vj[XSnZDDmc5IhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDN|LkS2JO69VS5? NYjqelY5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5NlM{QDNpPkK4PVI{Ozh|PD;hQi=>
MCF7 MonyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NE\kXIY1QCCqcoO= Mk\HRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkC4JO69VS5? MojkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7OEi2NlQoRjJ6OUi4OlI1RC:jPh?=
B16F10 NHKwR2JCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NY[0TJFMPDhiaILz Mo\YRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEMU\GNVAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNVIh|ryPLh?= M2LOWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUi4OlI1Lz5{OEm4PFYzPDxxYU6=
A549 NVTCWWR5S3m2b4TvfIlkcXS7IHHzd4F6 M1LiU|I1KGi{cx?= NFO2XHpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjd|IN88UU4> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTB{OEWzOEc,OjlyMki1N|Q9N2F-
A498 MkPORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGHUdGM1QCCqcoO= M1fsTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMUKuOUDPxE1w MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTB3N{C0Nkc,OjlyNUewOFI9N2F-
HuH7 M4\5VWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MV:0PEBpenN? MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi3SEegZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDJ3IN88UU4> NWXwVnJJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwOVcxPDJpPkK5NFU4ODR{PD;hQi=>
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HT-29 M33De2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkXqOFghcHK| M1XiXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwMEKg{txONg>? NX70NYM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PTZpPkK5OFA4QTV4PD;hQi=>
MIAPaCa2 MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NX7OcXBmPDhiaILz NHjGZY9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkA1QCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlA{KM7:TT6= M{nZZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVU3Lz5{OUSwO|k2PjxxYU6=
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A549 M1PDZ2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MYe0PEBpenN? MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDoeY1idiCDNUS5JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvODRizszNMi=> Ml3oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MEe5OVYoRjJ7NEC3PVU3RC:jPh?=
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SCC-4 MV\Hdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? NEXl[HdKdmirYnn0bY9vKG:oIHj1cYFvKFOFQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1QS53NkCyJO69VS5? M2LyTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
RKO NVPwU4ZuT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= NWKxWGtxUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ6Njh|NU[g{txONg>? NHnyRlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTNxJ{7TRW5ITVJ:L3G+
アッセイ
Methods Test Index PMID
Western blot Cleaved PARP / PARP ; P-Raf-1 / t-Raf-1 / p-MEK / t-MEK / p-ERK / t-ERK / p-PI3K / t-PI3K / p-AKT / AKT ; p-STAT3 / STAT3 / PTPMeg2 / p-EGFR / EGFR / pJAK2 / JAK2 / Bcl2 / Bcl-xl / Survivin 27508092 24019973
Immunofluorescence β-catenin ; E-cadherin / Vimentin 25209444 19825949
Growth inhibition assay Cell viability ; IC50 30377412 17671085
体内試験 At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. [1] Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. [5]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

  • Kinase assays:

    96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colorimetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes.

細胞試験:

[2]

  • 細胞株:A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells
  • 濃度: 30 nM-20 μM
  • 反応時間:72 hours
  • 実験の流れ:

    Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software.

動物試験:

[6]

  • 動物モデル:Male 5-week-old BALB-nu/nu mice with HPAC cells
  • 投薬量:50 mg/kg
  • 投与方法:Oral administration

溶解度 (25°C)

体外

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):
5% 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。

3mg/mL

化学情報

分子量 393.44
化学式

C22H23N3O4

CAS No. 183321-74-6
Storage 3年 -20°C
2年 -80°C in solvent
Smiles COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC

投与溶液組成計算機(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)

mg/kg g μL

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
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting Drug: Erlotinib Hydrochloride Cirrhosis Liver University of Texas Southwestern Medical Center July 2022 Phase 2
NCT03460678 Terminated Drug: Pemetrexed|Drug: Erlotinib Carcinoma Non-Small-Cell Lung Hikma Pharmaceuticals LLC February 28 2018 Phase 4
NCT02942095 Active not recruiting Drug: Ixazomib|Drug: Erlotinib Solid Tumors M.D. Anderson Cancer Center|Millennium: The Takeda Oncology Company March 6 2017 Phase 1
NCT02991651 Suspended Drug: IRX4204|Drug: erlotinib Lung Cancer Nonsmall Cell Io Therapeutics|Dartmouth College May 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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。

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よくある質問(FAQ)

質問1:
Can you please give me some advice for which solvent we should use to dissolve it for animal studies?

回答
For in vivo application, we recommend to use 5% DMSO+45% PEG 300+ddH2O up to 6mg/ml.

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