Erlotinib HCl (OSI-744)

For research use only. Not for use in humans.

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

Erlotinib HCl (OSI-744) Chemical Structure

CAS No. 183319-69-9

Erlotinib HCl (OSI-744, CP358774, NSC 718781)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。

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 2211.3 现货
RMB 3012.92 现货
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客户使用Selleck生产的Erlotinib HCl (OSI-744)发表文献410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 Erlotinib HCl (OSI-744, CP358774, NSC 718781)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 NXLVN2g4TnWwY4Tpc44h[XO|YYm= NYnvVJJTUW6qaXLpeIlwdiCxZjDISXIzKGmwIHj1cYFvKFONQmKzJINmdGy|IHL5JGhVWkZiYYPzZZktKEmFNUC9NU45QSEQvF2u MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQThzNUSxNkc,OTl6MUW0NVI9N2F-
human A431 cells NYe3SWk{TnWwY4Tpc44h[XO|YYm= NELIeW9KdmirYnn0bY9vKG:oIFXHSnIhcW5iaIXtZY4hSTR|MTDj[YxteyCkeTDIWHJHKGG|c3H5MEBKSzVyPUCuOFIh|ryPLh?= NXTDcpFVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4NVU1OTJpPkG5PFE2PDF{PD;hQi=>
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HepG2 NGjINVVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M{TyNVQ5KGi{cx?= MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB3Lkig{txONg>? MofXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OU[3NFgoRjJ4OEm2O|A5RC:jPh?=
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A549 MnHwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MkK3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJZq[WKuZTDj[YxteyCjZoTldkA1QCCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDZwMk[g{txONg>? M{n4[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEe5N|E1Lz5{Nki3PVMyPDxxYU6=
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MIAPaCa M1yxR2Z2dmO2aX;uJIF{e2G7 M3TyPWlvcGmkaYTpc44hd2ZiRWLCZlIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1KSVCjQ3GgZ4VtdHNiYomgSWxKW0FuIFnDOVAhRSB4LkezJO69VS5? NEL4U5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEixO|UzOyd-MkC4NVc2OjN:L3G+
NCI-H358 M{T2RmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXjGW5pJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN3ODDj[YxteyCjc4Pld5Nm\CCjczD2bYFjdGViY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA3Njh3IN88UU4> NXHvOVRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4O|k{OTRpPkK2PFc6OzF2PD;hQi=>
NCI-H1975 M1PJSWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MWO3NkBpenN? NWew[W9ESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKFR5OUDNJI12fGGwdDDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iNj65JO69VS5? NGDLTmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG4N|c1Oid-MkSxPFM4PDJ:L3G+
NCI-H1975 MljpRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2XEV|czKGi{cx?= NFP6UpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIdm\mm2aX7pZk1z\XOrc4ThcpQhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTC3MlA3KM7:TT6= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4NUm2PUc,OjR3NkW5Olk9N2F-
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A549 MmjpRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIjicJU1QCCqcoO= MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDjZ4s5KGG|c3H5MEBKSzVyIE2gO{4{PSEQvF2u M3Hab|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkO0PFg4Lz5{N{KzOFg5PzxxYU6=
NCI-H1975 NXGzZpJ2S3m2b4TvfIlkcXS7IHHzd4F6 Mo\yOFghcHK| Mk\GR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUhzOUe1JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB5LkS5PEDPxE1w NIjsOWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFg{OCd-MkS5NFA5OzB:L3G+
HCC827 NH;nbnRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NV3JfZdvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR2M5OjdiY3XscJMh[W[2ZYKgbJJ{KGK7IFHUVEBkd262ZX70JIF{e2G7LDDJR|UxKD1iNz61JO69VS5? M1PmclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUSzO|c5Lz5{MEG0N|c4QDxxYU6=
A549 Mk\0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M1T5[VczKGi{cx?= NX76XplESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJJVv\GW{IH7vdo1wgGmjIHPvcoRqfGmxboOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IEeuOVkh|ryPLh?= NWXtZXNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OlgxPDRpPkK1OFY5ODR2PD;hQi=>
BxPC3 NUC0cHpySW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGG5OoZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFL4VGM{KGOnbHzzJIFnfGW{IHjyd{BjgSCDVGCgZ49vfGWwdDDhd5NigSxiSVO1NEA:KDdwNjFOwG0v MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF2M{e3PEc,OjBzNEO3O|g9N2F-
NCI-H1975 Mo\nSpVv[3Srb36gZZN{[Xl? NEfOOW8zKGi{cx?= NEfWVm9KdmirYnn0bY9vKG:oIFXHSnIhVDh3OGKvWFk4OE1iZH;1ZoxmKG23dHHueEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUmNKNUhzOUe1JINmdGy|IHHmeIVzKDJiaILzJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDdwNjFOwG0v Mn7qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{C5PVQoRjJ|OUOwPVk1RC:jPh?=
PCI35 M3n2[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkDQO|IhcHK| NH3NNVdIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBRS0l|NTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS0ONLUigZZN{[XluIFnDOVAhRSB5Lkeg{txONg>? NVjvZYJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OFc3QTBpPkK2OVQ4PjlyPD;hQi=>
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SW962 NF3mWGVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJR|UxKD1iM{WuO|IyPyEQvF2= M3nTOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
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GI-ME-N MofpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3JR|UxKD1iNEiuNVM5PCEQvF2= NFvkS3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PTNxJ{7TRW5ITVJ:L3G+
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Met / Met / p-Axl / Axl / pERK / ERK / pEGFR / EGFR / p-STAT3 / STAT3 / p-Akt / Akt; 

PubMed: 28604685     


(b) Patient derived primary GBM neurospheres (GBM9) were exposure to erlotinib (1µM) for the indicated times followed by Western blot with the indicated antibodies. (c–d) A similar experiment in patient derived GBM neurospheres from two different patients (GBM39 and SK987). (e) U87EGFR cells were treated with erlotinib (1µM) for the indicated times followed by Western blot with the indicated antibodies. (f) Similar experiment was conducted in U87EGFRvIII cells.

p-Raf-1 / Raf-1 / p-MEK / MEK; 

PubMed: 27508092     


Cells from both ER and ECR groups were treated with 3 μM erlotinib for 72 h. Cell lysates were used for Western blotting with indicated antibodies.

cleaved PARP / PARP; 

PubMed: 27508092     


HCC827 or H1650 cells were treated with DMSO, celecoxib, erlotinib alone, or in combination for 48 h. Western blot analysis showed that cleaved PARP was higher in cells after combination treatment.

p27 / pS10-p27 / pT157-p27 / pT187-p27; 

PubMed: 21045138     


BT-474 and SK-BR-3 cells were treated with erlotinib at 0, 1, or 3 µM for 72 h, after which expression of total p27, p27 phosphorylated at S10 (pS10-p27), pT157-p27, and pT187-p27 was assessed by western blot analysis. β-actin was used as a loading control. 

Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Bad / Bim EL / PUMA; 

PubMed: 17927446     


Effects of erlotinib treatment on proapoptotic and antiapoptotic proteins in H3255 cells. H3255 cells were treated with different concentrations of erlotinib for 24 h. Cell lysates were examined by immunoblotting using antibodies specific for the indicated proteins.

28604685 27508092 21045138 17927446
Immunofluorescence
Bax / Cyto C; 

PubMed: 17927446     


Erlotinib induces colocalization of BAX and cytochrome c in PC-9 cells undergoing apoptosis. Cells were grown in Lab-Tek II chambers and treated with 100 nM erlotinib or DMSO for 48 h, fixed and immunostained with antibodies against BAX (green) and cytochrome c (red) or with DAPI to detect DNA (blue). Cells were imaged by confocal microscopy.

E-cadherin / β-catenin / Vimentin; 

PubMed: 19825949     


SUM149 cells were plated in 3D culture without or with erlotinib for 4 days. Immunofluorescence analysis was performed to detect E-cadherin, β-catenin, and vimentin. Nuclei were visualized with DAPI.

EGFR ; 

PubMed: 27612423     


HCC827 (delE746-A750), NCI-H3255 (L858R) and NCI-H1975 (L858R/T790M) cells were treated either with DMSO (control) or with 3 μM erlotinib/200 nM AZD9291 for the indicated time points. Cells were fixed and stained with EGFR antibody (red) and DAPI (blue, DNA dye) as described in the Materials and Methods. Representative images showing decreased EGFR immunofluorescence in erlotinib-sensitive HCC827 and NCI-H3255 cells. AZD9291 also reduced EGFR immunofluorescence even in NCI-H1975 cells. Scale bars, 10 μm. 

17927446 19825949 27612423
Growth inhibition assay
Cell viability; 

PubMed: 30377412     


a The MTT assay for PANC-1 viability. Different doses of erlotinib were added to the medium of PANC-1 cells. b LDH release was used to evaluate the cell death in PANC-1 cells in the presence of erlotinib. c The MTT assay for PaCa-2 cells in the presence of erlotinib treatment. d LDH release was used to evaluate the cell death in PaCa-2 cells in the presence of erlotinib.

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[6]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 4 mg/mL warmed (9.3 mM)
Water Insoluble
Ethanol 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):
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 粉状
溶于溶剂
别名 CP358774, NSC 718781

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