Erlotinib (OSI-774) HCl

目录号:S1023 别名: CP358774, NSC 718781 中文名称:盐酸厄洛替尼

仅限科研使用

Erlotinib (OSI-774, CP358774, NSC 718781) HCl是一种EGFR抑制剂,在无细胞试验中IC50为2 nM,对EGFR的选择性比对人c-Src或v-Abl高1000多倍。

Erlotinib (OSI-774) HCl Chemical Structure

CAS: 183319-69-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1564.29 现货
RMB 1183.19 现货
RMB 3012.92 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Erlotinib (OSI-774) HCl发表文献503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 Erlotinib (OSI-774, CP358774, NSC 718781) HCl是一种EGFR抑制剂,在无细胞试验中IC50为2 nM,对EGFR的选择性比对人c-Src或v-Abl高1000多倍。
靶点
HER1/EGFR [1]
(Cell-free assay)
2 nM
体外研究

Erlotinib作用于HNS人头部和颈部肿瘤细胞,有效抑制EGFR自磷酸化,HNS人头部和颈部肿瘤细胞是表达高水平EGFR的细胞系。[1] Erlotinib对SBC-5细胞增殖没有作用效果。相反, Erlotinib 显著抑制PC-9细胞增殖,这种作用存在剂量依赖性,PC-9细胞在EGFR基因第19外显子含缺失突变。Erlotinib处理也不会影响SBC-5细胞迁移。[2] Erlotinib 抑制HPAC细胞和Capan-1细胞生长, IC50 分别为1.1和3µM。10 uM Erlotinib 抑制EGFR在 Y845 (Src依赖性磷酸化) 和和Y1068(自磷酸化)位点磷酸化。[3] Erlotinib 只有作用于最敏感的细胞株时,抑制细胞外信号调节激酶, Akt, 和S6。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SKBR3 cells MoTXSpVv[3Srb36gZZN{[Xl? MVvJcohq[mm2aX;uJI9nKEiHUkKgbY4hcHWvYX6gV2tDWjNiY3XscJMh[nliSGTSSkBie3OjeTygTWM2OD1zLki5JO69VS5? Ml;UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6MUW0NVIoRjF7OEG1OFEzRC:jPh?=
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HT-29 Mnm4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MkPSO|IhcHK| M4\jUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36geY5l\XJibn;ycY95cWFiY3;u[Il1cW:wczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMj65PEDPxE1w NETibpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS2PFA1PCd-MkW0OlgxPDR:L3G+
PANC1 NV;kSGtCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWLt[llQPzJiaILz Mlv2S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gVGFPSzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNEUy16IHHzd4F6NCCLQ{WwJF0hOy5zIN88UU4> NEnPcXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW0O|Y6OCd-Mk[1OFc3QTB:L3G+
SCC25 NXjQWJhRSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NUK0TmQ5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTR2MzPSClZXzsd{whUUN3MDC9JFMvOzRizszNMi=> M3\uflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUSzO|c5Lz5{MEG0N|c4QDxxYU6=
NCI-H358 M4DOZmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1\TN|Q5KGi{cx?= NFnM[FJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzV6IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB2ODDodpMh[nliY3PrPEBie3OjeTygTWM2OCB;IEOuPVEh|ryPLh?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzJ|NEi4O{c,Ojd{M{S4PFc9N2F-
COS7 NYPFbWlQTnWwY4Tpc44h[XO|YYm= NIfWToxKdmirYnn0bY9vKG:oIHj1cYFvKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5Nm\CCrbjDDU3M4KGOnbHzzMEBKSzVyIE2gOEDPxE1w MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzF5OEeyNkc,OTdzN{i3NlI9N2F-
L3.6PL MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVS3NkBpenN? NIfQV5hIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBNOy54UFygZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iNDFOwG0v M3rlWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUS3OlkxLz5{NkW0O|Y6ODxxYU6=
HT-29 NGftXZhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NYfu[IhpPzJiaILz NX;Rfmx3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckB2dmSncjDofZBwgGmjIHPvcoRqfGmxboOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IESuN|ch|ryPLh?= M37mO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NE[4NFQ1Lz5{NUS2PFA1PDxxYU6=
OVCAR3 MoDRRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUW3NkBpenN? MnfaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTC0MlYh|ryPLh?= NYTyfnFxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1PVk2OzJpPkK2OVk6PTN{PD;hQi=>
Calu3 NV\jVXA5SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4jVfVczKGi{cx?= M3\ifmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HseVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncjDicJVmKGG|c3H5MEBKSzVyIE2gOE44KM7:TT6= M4PGR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUm5OVMzLz5{NkW5PVU{OjxxYU6=
hematopoietic progenitor cell Mn3GS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3jDfGdzd3e2aDDpcohq[mm2aX;uJI9nKEqDS{KgWlYyP0ZibYX0ZY51KGW6cILld5NqdmdiaHXtZZRweG:rZYTpZ{Bxem:pZX7peI9zKGOnbHzzJIl{d2yjdHXkJIZzd21icH;sfYN6fGinbXnhJJZmemFicHH0bYVvfCCkeTDjc4xwdnliZn;ycYlv\yCjc4PhfUwhUUN3MDC9JFUh|ryPLh?= NX\zdXJJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexO|g4OjJpPkG3NVc5PzJ{PD;hQi=>
KB Ml25RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2\xdFQ5KGi{cx?= M2XMd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1KgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKGGwZDDTdoMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFUh|ryPLh?= M{D3[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUi4OlIxLz5{NkG4PFYzODxxYU6=
N87 MYrGeY5kfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKEW{YlKyJIlvfHKjY3XscJVt[XJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE56NzDj[YxteyCkeTDFUGlUSSxiSVO1NEA:KDVwMjFOwG0v Mk\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NE[2OVUoRjJyM{S2OlU2RC:jPh?=
NCI-H1975 MY\DfZRwfG:6aXPpeJkh[XO|YYm= NGK3dFA4OiCqcoO= NU\vfHp{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixPVc2KGOnbHzzJIV5eHKnc4PpcochTUeIUjDMPFU5Wi:WN{mwUUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEWuOVEh|ryPLh?= NHjPXY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxNVEzOyd-MkS0NVEyOjN:L3G+
MRC5 NWPvbnRUSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmnMO|IhcHK| NGjVU5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3SR|Uh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTC1Mlgh|ryPLh?= MojvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3OUm1N|IoRjJ4NUm5OVMzRC:jPh?=
HepG2 NHjldGFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NWXtdIc2PDhiaILz NX21fpZXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOU45KM7:TT6= MoXTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OU[3NFgoRjJ4OEm2O|A5RC:jPh?=
NCI-H358 MVzBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYj1cVg5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN3ODDj[YxteyCjZoTldkBpenNiYomgRXRRKGOxboTlcpQh[XO|YYmsJGlEPTBiPTC2JO69VS5? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF2M{e3PEc,OjBzNEO3O|g9N2F-
A549 M4nGSWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1zveWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{B3cWGkbHWgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSB4LkK2JO69VS5? NWjQXWo{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4O|k{OTRpPkK2PFc6OzF2PD;hQi=>
LNCAP NFO5V49EgXSxdH;4bYNqfHliYYPzZZk> M4PMXFQh\GG7cx?= M{LZ[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGGodHXyJFQh\GG7czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3MDC9JFYvPjNizszNMi=> NWn6UXMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOlk3ODFpPkKyNVY6PjBzPD;hQi=>
MIAPaCa M4fOU2Z2dmO2aX;uJIF{e2G7 MoDHTY5pcWKrdHnvckBw\iCHUlLiNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWlCWGGFYTDj[YxteyCkeTDFUGlUSSxiSVO1NEA:KDZwN{Og{txONg>? NGTiU5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEixO|UzOyd-MkC4NVc2OjN:L3G+
NCI-H358 Mn7nRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mn64RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFM2QCClZXzsd{Bie3Onc4Pl[EBieyC4aXHicIUh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTC2Mlg2KM7:TT6= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh5OUOxOEc,OjZ6N{mzNVQ9N2F-
NCI-H1975 MVPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHzMdVA4OiCqcoO= NECyT4VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOTl5NTDj[YxteyCneIDy[ZN{cW6pIFXHSnIhXDd7MF2gcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB4Lkmg{txONg>? M1L1N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUizO|QzLz5{NEG4N|c1OjxxYU6=
NCI-H1975 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mli5O|IhcHK| MmPuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDn[YZqfGmwaXKtdoV{cXO2YX70JIh2dWGwIF7DTU1JOTl5NTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iNz6wOkDPxE1w M37EcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NU[1PVY6Lz5{NEW2OVk3QTxxYU6=
A549 M2HsZmN6fG:2b4jpZ4l1gSCjc4PhfS=> MonrOFghcHK| M2PtfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFcvODl7IN88UU4> NX6zbmpMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5OzBpPkK0PVAxQDNyPD;hQi=>
A549 Mn[0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4TmWVQ5KGi{cx?= NFzoTo5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBk[2t6IHHzd4F6NCCLQ{WwJF0hPy5|NTFOwG0v NUnUU4FPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkeyN|Q5QDdpPkK3NlM1QDh5PD;hQi=>
NCI-H1975 NWfBTFhmS3m2b4TvfIlkcXS7IHHzd4F6 MnjwOFghcHK| MnLIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB5LkS5PEDPxE1w NWe4XYFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA5OzBpPkK0PVAxQDNyPD;hQi=>
HCC827 NF3RNHpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MkSzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ1O4Nlch[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwJF0hPy53IN88UU4> M2LpNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUSzO|c5Lz5{MEG0N|c4QDxxYU6=
A549 M{HKNWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M3TqSVczKGi{cx?= M{Dac2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjD1coRmeiCwb4Ltc5hq[SClb37kbZRqd26|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB5LkW5JO69VS5? NH;wd3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS2PFA1PCd-MkW0OlgxPDR:L3G+
BxPC3 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1jGXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQojQR|Mh[2WubIOgZYZ1\XJiaILzJIJ6KEGWUDDjc451\W62IHHzd4F6NCCLQ{WwJF0hPy54IN88UU4> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF2M{e3PEc,OjBzNEO3O|g9N2F-
NCI-H1975 NUTSfmI2TnWwY4Tpc44h[XO|YYm= NWf1em9[OiCqcoO= NHjpZoZKdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKvWFk4OE1iZH;1ZoxmKG23dHHueEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUmNKNUhzOUe1JINmdGy|IHHmeIVzKDJiaILzJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDdwNjFOwG0v MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|MEm5OEc,OjN7M{C5PVQ9N2F-
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HepG2 MmH1R5l1d3SxeHnjbZR6KGG|c3H5 M3HQO|I1KGi{cx?= NGrFTnlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB{NDDodpMh[nlic4DlZ5Rzd3Cqb4TvcYV1enluIFnDOVAhRSB{NTFOwG0v MlSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2OEexNlcoRjJ6NEi3NVI4RC:jPh?=
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MDA-MB-231 NHnxfFFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1iyRlczKGi{cx?= M3fqN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA{OC5zMjFOwG0v M{HsclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUKzN|g{Lz5{OEmyN|M5OzxxYU6=
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MDA-MB-231 NHLibGdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Ml\YOFghcHK| NFvP[YlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOzNwNE[g{txONg>? NIW2RYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmyN|M5Oyd-Mki5NlM{QDN:L3G+
MDA231 M1LqPGN6fG:2b4jpZ4l1gSCjc4PhfS=> NXvaU4RsPCCmYYnz M3[0W2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTJ|MTDj[YxteyCjZoTldkA1KGSjeYOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUCgQUA{PC53IN88UU4> M1fudlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MU[5OlAyLz5{MkG2PVYxOTxxYU6=
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HEK293 NI\IOm1HfW6ldHnvckBie3OjeR?= M3fGeFUhdWmwcx?= NXP2e2hIUW6qaXLpeIlwdiCxZjDoeY1idiCuaY\ldkBQSVSSMVKzJIV5eHKnc4Pl[EBqdiCKRVuyPVMhTmyyLVnuJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCdM1jdSVE4NWKndHHHJJVxfGGtZTDpcoN2[mG2ZXSg[o9zKDVibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBMcSB;IESxJO69VSxiSVO1NEA:KDR2IN88UU4> NX7ZcYxnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFExPjhpPkKyOVQyODZ6PD;hQi=>
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Assay
Methods Test Index PMID
Western blot p-Met / Met / p-Axl / Axl / pERK / ERK / pEGFR / EGFR / p-STAT3 / STAT3 / p-Akt / Akt p-Raf-1 / Raf-1 / p-MEK / MEK cleaved PARP / PARP p27 / pS10-p27 / pT157-p27 / pT187-p27 Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Bad / Bim EL / PUMA 28604685 27508092 21045138 17927446
Immunofluorescence Bax / Cyto C E-cadherin / β-catenin / Vimentin EGFR 17927446 19825949 27612423
Growth inhibition assay Cell viability 30377412
体内研究 Erlotinib单独作用于H460a肿瘤模型,抑制肿瘤生长,这种作用存在剂量依赖性,与药物的循环水平相关。

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]
  • 激酶实验:

    每孔使用100 μL 溶于PBS的0.25 mg/mL PGT对96孔板包被,然后在37oC温育过夜。吸取移除过量PGT,使用冲洗 buffer (0.1% Tween-20,溶于PBS)清洗实验板3次。在 50 μL 50 mM HEPES (pH 7.3), 含125 mM NaCl, 24 mM MgCl2, 0.1 mM 原钒酸钠, 20 μM ATP, 1.6 μg/mL EGF, 以及从A431细胞膜上亲和纯化的15 ng EGFR的混合物中进行激酶反应。加入溶于 DMSO的 Erlotinib,DMSO 终浓度为2.5%。加入ATP,开始磷酸化,在室温下进行8分钟,且持续震荡。加入吸取的反应混合物,激酶反应终止,使用冲洗 buffer冲洗4次。磷酸化的PGT与50 μL每孔 HRP联合的PY54 抗磷酸抗体[在封闭液(3% BSA 和0.05% Tween-20,溶于 PBS)中稀释到0.2 μg/mL]温育25分钟后,测量磷酸化的PGT。吸取移除抗体,使用冲洗buffer冲洗实验板4次。加入 TMB 微孔过氧化物酶底物,每孔50μL,进行比色分析,然后加入0.09 M 硫酸,每孔50 μL,终止反应。在450 nm处测定吸光值而测定磷酸化。

细胞实验:[3]
  • Cell lines: HPAC细胞系和Capan-1细胞
  • Concentrations: 0.01 μM-10 μM
  • Incubation Time: 4天或6天
  • Method: 为了测评对细胞增殖的抑制作用,进行MTT实验。细胞在96孔板上在37oC下预温育,单独加入Erlotinib 和Gemcitabine,或者联合加入。在37oC下处理4天(HPAC细胞)或6天(Capan-1 细胞)后,每孔加入10 mL MTT,然后在37oC下温育2-5小时。使用Benchmark Plus 酶标仪在450和600 nm处测定每孔的光密度。每组每种药物实验独立重复进行2次或3次。按如下计算细胞增殖抑制百分数: [(药物处理孔中的平均吸光值-无细胞孔中平均吸光值)/(对照组孔中平均吸光值-无细胞孔中平均吸光值)] × 100。
动物实验:[6]
  • Animal Models: 携带HPAC细胞的雄性5周大的BALB-nu/nu小鼠
  • Dosages: 50 mg/kg
  • Administration: 口服处理

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):
15% Captisol

16 mg/mL warmed (suspension)

* 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 429.90
化学式

C22H23N3O4.HCl

CAS号 183319-69-9
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
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 Recruiting Drug: IRX4204|Drug: erlotinib Lung Cancer Nonsmall Cell Io Therapeutics|Dartmouth College May 2016 Phase 1

(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:
Whether S1023 is suitable for mouse assays?

回答:
Dissolving S1023 in 15% Captisol is for oral gavage and it's a suspension.