Osimertinib (AZD9291)

For research use only. Not for use in humans.

目录号:S7297

Osimertinib (AZD9291) Chemical Structure

CAS No. 1421373-65-0

Osimertinib (AZD9291) 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。

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客户使用Selleck生产的Osimertinib (AZD9291)发表文献197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 Osimertinib (AZD9291) 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
PC9 GR4 Mm\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHoUZVpOC1zMDFOwG0> MX[3NkBp M1rlRolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MUmyOVk1QDZ|Mx?=
PC9 M4XBfWZ2dmO2aX;uJGF{e2G7 MoPtNE0yOCEQvF2= NWGwRW15PzJiaB?= MnnYbY5pcWKrdIOgW3QhTUeIUjDheEBtd3diY3;uZ4VvfHKjdHnvcpM> MWSyOVk1QDZ|Mx?=
PC9 GR4 MkXuSpVv[3Srb36gRZN{[Xl? NXvKXFRjOC1zMDFOwG0> NYfGR45SPzJiaB?= MWHpcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA> MnzmNlU6PDh4M{O=
VP-2 MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoftOVAhdk1? MojDNVAh\A>? M1r4eGROW09? MXzpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? NHmxWokzPTR5N{OyOS=>
PC-9/ERc1 NILlNVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[zZ|UxKG6P NHjZWpoyOCCm NUPpN3VsTE2VTx?= NGC0bYdqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= M123[VI2PDd5M{K1
PC-9/BRc1 NY[4UHRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP6OVAhdk1? M3zVVVExKGR? MoHKSG1UVw>? M1jJ[YlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= NV;R[XlZOjV2N{ezNlU>
VP-2 M4\IW2Z2dmO2aX;uJGF{e2G7 MlfKOVAhdk1? Ml;WNlQhcA>? MXjEUXNQ NVjGXWx[cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> MUWyOVQ4PzN{NR?=
PC-9/ERc1 NGLzZ5hHfW6ldHnvckBCe3OjeR?= NYfmNHI5PTBibl2= NHSzbnMzPCCq MUXEUXNQ MVrpcoR2[2W|IHX4dJJme3Orb36gc4YhfGinIIDyc4Fxd3C2b4TpZ{BDS0xvMjDmZY1qdHlibXXtZoVzKEKLTR?= NHHTfnczPTR5N{OyOS=>
PC-9/BRc1 M33ifWZ2dmO2aX;uJGF{e2G7 NEPHWoI2OCCwTR?= NX3sd2hZOjRiaB?= MnTnSG1UVw>? MkjUbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= NVKzN5dFOjV2N{ezNlU>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-EGFR / p-AKT / p-ERK; 

PubMed: 28416483     


PC-9/BRc1 cells were treated with the indicated doses of osimertinib. Drugs were refreshed every 24 hours. Cellular lysates were probed with the indicated antibodies. Osim: osimertinib.

ABCB1; 

PubMed: 27649127     


The effect of osimertinib at 0.3 μM on the expression of ABCB1 was measured in KB-3-1 and KB-C2 cell lines for 0, 24, 48, and 72 h.

28416483 27649127
Growth inhibition assay
Cell viability; 

PubMed: 31043587     


Cells were treated with gefitinib or osimertinib for 72 h. Cell viability was measured by MTT assay. *P < 0.05, **P < 0.01, ***P < 0.005 by t-test.

31043587
Immunofluorescence
Ki67 / γH2AX / p16; 

PubMed: 29212784     


PC9ER cells were treated for 5 days with either 3×mAbs (20 μg/ml), saline (CTRL), or with a low dose of osimertinib (2.5 nM). Shown are representative images of cells fixed in paraformaldehyde and immunostained for KI67 (panel E), γH2AX (panel F), and p16 (panel G). DAPI counterstaining was used to follow nuclear localization. Scale bar, 20 μm. The box and whisker plots, where the ends of the box are the upper and lower quartiles, depict quantifications of results obtained in three independent experiments. **P ≤ 0.01, ***P ≤ 0.001, n = 4; one-way ANOVA with Tukey's test.

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]

- 合并
  • Animal Models: PC9和H1975移植瘤小鼠
  • Dosages: ~5 毫克/千克
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 99 mg/mL warmed (198.15 mM)
Ethanol 43 mg/mL warmed (86.06 mM)
Water 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):
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 粉状
溶于溶剂
别名 N/A

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

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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 Active not recruiting Drug: AZD9291 Non Small Cell Lung Cancer Hellenic Oncology Research Group August 2 2016 Phase 2
NCT02511106 Active not recruiting Drug: AZD9291 80 mg/40 mg|Drug: Placebo AZD9291 80 mg/40 mg Stage IB-IIIA Non-small Cell Lung Carcinoma AstraZeneca October 21 2015 Phase 3
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

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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: 1% DMSO+30% PEG 300+dd H2O at up to 30mg/ml.

EGFR Signaling Pathway Map

相关EGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID