Osimertinib (AZD9291)

目录号:S7297

Osimertinib (AZD9291) Chemical Structure

Molecular Weight(MW): 499.61

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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RMB 807.34 现货
RMB 1105.43 现货
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客户使用该产品的4个实验数据:

  • Lysates from MGH121 parental cells treated with 1 μM of the indicated TKIs except for AZD9291 (160 nM) for 6 hours were probed with the indicated antibodies.

    Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 . Osimertinib (AZD9291) purchased from Selleck.

    Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.

    Cancer Res, 2017.. Osimertinib (AZD9291) purchased from Selleck.

  • F, PC-9/ffluc and PC-9/LMC-GR cells (2×103 cells/well) were incubated with various concentrations of osimertinib for 72 hours. Cell viability was determined by MTT assay. Bars represent SD of quadruplicate cultures. Data shown are representative of three independent experiments with similar results.

    Mol Cancer Ther, 2017, 16(3):506-515. Osimertinib (AZD9291) purchased from Selleck.

    Western blot analysis showing phospho-EGFR (p-EGFR), total EGFR, phospho-ERK (p-ERK), total ERK, phospho-AKT (p-AKT), total AKT and β-actin as a loading control in H1975 cells treated with the indicated inhibitors. Equivalent amounts of proteins from whole cell lysates were subjected to WB analysis to detect the indicated proteins.

    J Biol Chem, 2015, 290(28): 17495-504. Osimertinib (AZD9291) purchased from Selleck.

产品安全说明书

EGFR抑制剂选择性比较

生物活性

产品描述 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 M3rOTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljaNE0yOCEQvF2= M36zUFczKGh? MmP3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnyzNlU6PDh4M{O=
PC9 NIfzT4dHfW6ldHnvckBCe3OjeR?= NFjiZY0xNTFyIN88US=> MkfiO|IhcA>? MkPzbY5pcWKrdIOgW3QhTUeIUjDheEBtd3diY3;uZ4VvfHKjdHnvcpM> MlPuNlU6PDh4M{O=
PC9 GR4 MUjGeY5kfGmxbjDBd5NigQ>? NHLtV3kxNTFyIN88US=> MYS3NkBp MVLpcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA> NGLJRpEzPTl2OE[zNy=>
VP-2 NInwbotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITiSlg2OCCwTR?= MlzRNVAh\A>? NIW3PFZFVVOR MYfpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? M2S3d|I2PDd5M{K1
PC-9/ERc1 NUTpZ3p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfGcWpYPTBibl2= M{\UbVExKGR? NUTPNphOTE2VTx?= M3XFb4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= MU[yOVQ4PzN{NR?=
PC-9/BRc1 MlLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjxZWg2OCCwTR?= MY[xNEBl NF7LdIxFVVOR NUfGN2RocW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz NF32Um0zPTR5N{OyOS=>
VP-2 NW\6Ro5GTnWwY4Tpc44hSXO|YYm= NHXNNJQ2OCCwTR?= MnqyNlQhcA>? NYfCcZRVTE2VTx?= MlK4bY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= M3W0TVI2PDd5M{K1
PC-9/ERc1 MYfGeY5kfGmxbjDBd5NigQ>? M1W0UFUxKG6P MVWyOEBp M2jNN2ROW09? MmjTbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= NUmzNo1ROjV2N{ezNlU>
PC-9/BRc1 NYTYSFY3TnWwY4Tpc44hSXO|YYm= Mn\lOVAhdk1? NUjsSYJlOjRiaB?= NGnHeWVFVVOR M2KzdYlv\HWlZYOg[ZhxemW|c3nvckBw\iC2aHWgdJJw[XCxcITveIlkKEKFTD2yJIZidWmueTDt[Y1j\XJiQlnN MkDkNlU1Pzd|MkW=

... Click to View More Cell Line Experimental Data

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]

+ 展开
  • Animal Models: PC9和H1975移植瘤小鼠
  • Formulation: --
  • 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 从左到右依次加入纯溶剂:
1% DMSO+30% PEG 300+ddH2O
30mg/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
稳定性 powder
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02923947 Not yet recruiting Solid Tumours AstraZeneca|Quintiles, Inc. January 2017 Phase 1
NCT02972333 Not yet recruiting EGFR-TKI Resistant Mutation|Nonsmall Cell Lung Cancer|AZD9291|Brain Metastases Shandong Cancer Hospital and Institute|AstraZeneca December 2016 Phase 3
NCT02997501 Recruiting Lung Cancer AstraZeneca|TigerMed December 2016 Phase 3
NCT02771314 Recruiting Non Small Cell Lung Cancer Hellenic Oncology Research Group June 2016 Phase 2
NCT02811354 Not yet recruiting Carcinoma, Non-Small-Cell Lung National University Hospital, Singapore|AstraZeneca|Singapore Clinical Research Institute June 2016 Phase 2
NCT02736513 Recruiting Lung Cancer Rabin Medical Center May 2016 Phase 2

技术支持

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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