Osimertinib (AZD9291)

目录号:S7297 别名: Mereletinib

仅限科研使用

Osimertinib (AZD9291, Mereletinib)是口服不可逆的,突变选择性EGFR抑制剂,在 LoVo细胞中对Exon 19 缺失的 EGFR,L858R/T790M EGFR,和 WT EGFR的IC50分别为12.92,11.44 和 493.8 nM。Phase 3。

Osimertinib (AZD9291) Chemical Structure

CAS: 1421373-65-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 647.05 现货
RMB 573.71 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Osimertinib (AZD9291)发表文献293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 Osimertinib (AZD9291, Mereletinib)是口服不可逆的,突变选择性EGFR抑制剂,在 LoVo细胞中对Exon 19 缺失的 EGFR,L858R/T790M EGFR,和 WT EGFR的IC50分别为12.92,11.44 和 493.8 nM。Phase 3。
特性 Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.
靶点
L858R/T790M EGFR [1]
(LoVo cells)
Exon 19 deletion EGFR [1]
(LoVo cells)
WT EGFR [1]
(LoVo cells)
11.44 nM 12.92 nM 493.8 nM
体外研究

与体外野生型相比,在突变EGFR 细胞系中AZD9291能更有效的抑制增殖。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC-9/BRc1 MYnGeY5kfGmxbjDBd5NigQ>? MomzOVAhdk1? MmjnNlQhcA>? M4rCRWROW09? NU\J[nM2cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NEG4ZmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O|MzPSd-MkW0O|c{OjV:L3G+
PC-9/ERc1 NEHzemhHfW6ldHnvckBCe3OjeR?= MnfYOVAhdk1? MUKyOEBp NWnOV2JTTE2VTx?= NWPFNYtGcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> M4DUNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEe3N|I2Lz5{NUS3O|MzPTxxYU6=
VP-2 NHe5OY1HfW6ldHnvckBCe3OjeR?= NGfsXGo2OCCwTR?= MYOyOEBp MVLEUXNQ MmDBbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC-9/BRc1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf1OVAhdk1? Mmn4NVAh\A>? M1Oy[GROW09? M1S4Z4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= NYG2e3pZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
PC-9/ERc1 NGjObJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnoOVAhdk1? NUjX[3J1OTBiZB?= NI\Wd2lFVVOR NUHwcVNFcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz NXXEc2lzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0O|c{OjVpPkK1OFc4OzJ3PD;hQi=>
VP-2 MmjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYm1NEBvVQ>? MXGxNEBl MXTEUXNQ NFfDdGJqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= NGjucI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O|MzPSd-MkW0O|c{OjV:L3G+
PC9 GR4 NYrRdJZlTnWwY4Tpc44hSXO|YYm= NGXnSpMxNTFyIN88US=> MWO3NkBp MkSxbY5pcWKrdIRCpGVITlJicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJJNq\26jbHnu[:Kh Ml:wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NEi2N|MoRjJ3OUS4OlM{RC:jPh?=
PC9 NXfKN3ZDTnWwY4Tpc44hSXO|YYm= NGO0WpUxNTFyIN88US=> MXS3NkBp MnTWbY5pcWKrdIOgW3QhTUeIUjDheEBtd3diY3;uZ4VvfHKjdHnvcpM> MnvMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NEi2N|MoRjJ3OUS4OlM{RC:jPh?=
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NCI-H1975 Mn;HRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NVXlRXlnPzJiaB?= M4rL[mlEPTBiPTCwMlAyODVizszN M{XvfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{G2OlQyLz5{OEexOlY1OTxxYU6=
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PC9-DRH MlrsSpVv[3Srb36gZZN{[Xl? MVOyJIg> NGfGfWFKSzVyIE2gNE4xOTNizszN MoPWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NU[yNlIoRjJ4N{W2NlIzRC:jPh?=
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HCC827 MXPGeY5kfGmxbjDhd5NigQ>? MWe5OkBp MlXQSWM2OCB;IECuNFE1KM7:TR?= NFjlcJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKyOVI3QSd-MkiyNlUzPjl:L3G+
HCC827 M2XRPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M4PNO|k3KGh? M3fZR2VEPTBiPTCwMlAyPCEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
NCI-H1975 MlzwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MkXFPVYhcA>? NIjUOYNGSzVyIE2gNE4xOTRizszN M1G0Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
NCI-H1975 M2PTdGZ2dmO2aX;uJIF{e2G7 M2\pdVIhcA>? NV7ydmlsUUN3MDC9JFAvODF3IN88US=> M2\T[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
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NCI-H1975 MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NGH1O284OiCq M2f2U2lEPTBiPTCwMlAyQSEQvF2= NYPM[nZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlY4PzNpPkK5OFY3Pzd|PD;hQi=>
NCI-H1975 M1Tob2Z2dmO2aX;uJIF{e2G7 MWW5OkBp M2X0XWVEPTBiPTCwMlAyQSEQvF2= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ{NUK2PUc,Ojh{MkWyOlk9N2F-
NCI-H1975 NILJfldCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MoP2PVYhcA>? NWLP[XlTTUN3MDC9JFAvODF7IN88US=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZyM{m5NUc,Ojh4MEO5PVE9N2F-
NCI-H1975 M3KyTmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MoTVO|IhcA>? NVz4fGhKUUN3MDC9JFAvODF7IN88US=> M1fYeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEWzN|QxLz5{OUi1N|M1ODxxYU6=
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human hepatocytes NXXoTJpCTnWwY4Tpc44h[XO|YYm= M2f4NGlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5iaIXtZY4hcGWyYYTvZ5l1\XNiYYPz[ZN{\WRicHXyJI1qdGyrb36gZ4VtdHN? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR{Nkm5Okc,Ojh2Mk[5PVY9N2F-
rat hepatocytes NUDlS21lTnWwY4Tpc44h[XO|YYm= NUDJc|VQUW62cnnud4lkKGOuZXHyZY5k\SCrbjDyZZQhcGWyYYTvZ5l1\XNiYYPz[ZN{\WRicHXyJI1qdGyrb36gZ4VtdHN? NFPLeJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESyOlk6Pid-Mki0NlY6QTZ:L3G+
A549, NCI-H1975 NGPqWIhHfW6ldHnvckBie3OjeR?= NYTXS5VPW2WuZXP0bZZqfHlicnH0bY8hd2ZiSVO1NEBnd3JiRVfGMZN1cW23bHH0[YQhf2muZDD0fZBmKEWJRmKgbY4hcHWvYX6gRVU1QSClZXzsd{B1dyCLQ{WwJIZweiCHR1\SJGw5PTiUL2S3PVBOKGSxdXLs[UBufXSjboSgbY4hcHWvYX6gUmNKNUhzOUe1JINmdGy| NF\QNJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
A549, PC9 M2nhTWZ2dmO2aX;uJIF{e2G7 Mmm3V4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhTUeILYP0bY12dGG2ZXSge4lt\CC2eYDlJGVITlJiaX6gbJVu[W5iQUW0PUBk\WyuczD0c{BKSzVyIH\vdkBGT0[UIHTlcIV1cW:wIH31eIFvfCCrbjDoeY1idiCSQ{mgZ4VtdHN? NXrqW|lMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVYzOjJpPkK2O|U3OjJ{PD;hQi=>
HCC827 NYDBT3VISXCxcITvd4l{KGG|c3H5 NFvm[FdKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjDR|gzPyClZXzsd{Bp[XKkb4LpcochTUeIUjDFO|Q3KHSxIFG3OVAh\GWuZYTpc44hdXW2YX70JIF{e2W|c3XkJIF{KGWjcnz5JIFxd3C2b4TpZ{Bk\WyuczDheEA{KHWPIHHmeIVzKDJ2IHjyd{BjgSCDbn7lfIlvKFZvRlnUR{9xem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6KCiUdnKgQUAyNjN2IITvJFEvPjdnKR?= NVHiR2FrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OVM{PDBpPkK5PFU{OzRyPD;hQi=>
NCI-H1975 NWPBPXFoTnWwY4Tpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKEWJRmKgUFg2QFJxVEe5NG0h\G:3YnzlJI12fGGwdDDwbI9{eGixconsZZRqd25iaX6gSWdHNXO2aX31cIF1\WRiaIXtZY4hVkOLLVixPVc2KGOnbHzzJIF1KDFidH:gNVAxKG6PIHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> M4\ENFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUC2NVE1Lz5{OUmwOlEyPDxxYU6=
A431 M1[0cGZ2dmO2aX;uJIF{e2G7 NHrmZ2lU\WynY4Tpeol1gSC{YYTpc{whemG2aX:gTWM2OCCob4KgbJVu[W5iQUSzNUBk\WyuczDveoVz\XiycnXzd4lv\yC5aXzkMZR6eGViRVfGVkB1dyCLQ{WwJIZweiCqdX3hckBPS0lvSEG5O|Uh[2WubIOg[ZhxemW|c3nu[{BGT0[UIGS3PVBON0x6NUjSJI12fGGwdB?= MnPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{G2N|koRjJ5MUOxOlM6RC:jPh?=
PC9 MXjBcpRqfHWvb4KgZYN1cX[rdImgZZN{[Xl? M1zVb2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDPUBk\WyuczDoZZJjd3KrbnegSWdHWiCneH;uJFE6KGSnbHX0bY9vKGGldHn2ZZRqdmdibYX0ZY51KHinbn;ndoFnfGWmIHnuJHNEUURibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiMUCgcYcwc2dxZHH5MEBxdyCzZDDmc5IhPyCmYYnzJJJmdGG2aY\lJJRwKGOxboTyc4w> NFzFTYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3NVk3Oyd-MkWyO|E6PjN:L3G+
A431 NXLINGppSW62aYT1cY9zKGGldHn2bZR6KGG|c3H5 MkH5RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUSzNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCVQ1nEJI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFUhdWdxa3ev[IF6NCCybzDx[EBnd3JiNzDkZZl{KHKnbHH0bZZmKHSxIHPvcpRzd2x? MoLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{G5OlMoRjJ3MkexPVY{RC:jPh?=
Assay
Methods Test Index PMID
Western blot p-EGFR / p-AKT / p-ERK ABCB1 28416483 27649127
Growth inhibition assay Cell viability 31043587
Immunofluorescence Ki67 / γH2AX / p16 29212784
体内研究 AZD9291(5mg / kg p.o.)引起整个EGFRm+(PC9)和EGFRm+/ T790M(H1975)肿瘤模型肿瘤中显著的肿瘤消退,伴随着对体内EGFR磷酸化和下游关键信号通路,如AKT和ERK的显著抑制。[2]

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)

动物实验:

[2]

  • Animal Models: PC9和H1975移植瘤小鼠
  • Dosages: ~5 毫克/千克
  • Administration: p.o.

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):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O

7.5mg/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 499.61
化学式

C28 H33 N7 O2

CAS号 1421373-65-0
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
NCT02841579 Completed Drug: Osimertinib Non-Small Cell Lung Cancer MedSIR|AstraZeneca August 2016 Phase 2
NCT02771314 Unknown status Drug: AZD9291 Non Small Cell Lung Cancer Hellenic Oncology Research Group August 2 2016 Phase 2
NCT02529995 Completed Drug: AZD9291 40 mg|Drug: AZD9291 80 mg Carcinoma Non-Small-Cell Lung With EGFR Mutation Positive AstraZeneca August 24 2015 Phase 1
NCT02491944 Completed Drug: AZD9291|Drug: [14C]AZD9291 Oncology AstraZeneca July 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

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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:
Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

回答:
Osimertinib can be used for animal study. The vehicle we suggest is: 5%DMSO+40%PEG300+5%Tween 80+50%ddH2O.