1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Osimertinib

Osimertinib  (Synonyms: 奥希替尼; AZD-9291; Mereletinib)

目录号: HY-15772 纯度: 99.96%
COA 产品使用指南

Osimtinib (AZD9291) 是一种共价结合、具有口服活性、不可逆和突变选择性的 EGFR 抑制剂,其有效抑制 L858R (IC50=12 nM) 和 L858R/T790M (IC50=1 nM) EGFR。Osimtinib 解决了肺癌 T790M 突变介导的 EGFR 抑制剂耐药。

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Osimertinib Chemical Structure

Osimertinib Chemical Structure

CAS No. : 1421373-65-0

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10 mM * 1 mL in DMSO ¥715
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5 mg ¥650
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50 mg ¥1700
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1 g ¥7800
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Customer Review

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 88 篇科研文献

Proliferation Assay
WB

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are treated with AZD9291 or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    Measurement of antiproliferation effects of AZD9291 by EdU incorporation assay.

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are exposed to indicated concentrations of AZD9291 for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

    Osimertinib purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595.  [Abstract]

    MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.  [Abstract]

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.  [Abstract]

    Effect of PCI-32765, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50, Enzyme assays)

    EGFRL858R/T790M

    1 nM (IC50, Enzyme assays)

    体外研究
    (In Vitro)

    Osimertinib (AZD9291) (0-10 μM;72 小时) 显著抑制细胞增殖,IC50 分别为 41、26、41 和 31 nM[2]
    Osimertinib (0-10 μM;72 小时) 抑制细胞增殖 (携带 T790M 突变、外显子 19del+T790M 或 L858R+T790M 的 Ba/F3 细胞),IC50 分别为 6、7 和 74 nM[2]
    Osimertinib 在两种 EGFR 细胞系:致敏突变体 (PC-9 的平均 IC50 为 8 nM) 和 T790M (H1975 和 PC-9VanR 的平均 IC50 为 11 和 40 nM) 中具有高表型效力[2]
    Osimertinib (0-10 μM;72 小时) 抑制携带 EGFR 外显子 20 插入突变的 Ba/F3 细胞,对于 A763_Y764insFQEA (FQEA)、Y764_V765insHH (HH)、A767_V769dupASV (ASV) 和 D770_N771insNPG (NPG) 细胞的 IC50 范围为 16 到 701 nM[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=6, 7, 74 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Dramatically inhibited cell proliferation (IC50s=41, 26, 41, 31 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=16, 701, 230, 38 nM, respectively)

    Apoptosis Analysis[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
    Concentration: 0.1 μM
    Incubation Time: 48 hours
    Result: Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.
    体内研究
    (In Vivo)

    Osimertinib (0.1-25 mg/kg;口服每日一次,持续 14 天) 在 PC-9 (ex19del) 和 H1975 (L858R/T790M) 肿瘤异种移植模型中诱导显著的剂量依赖性消退[1]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
    Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
    Administration: p.o.; daily for 14 days
    Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
    Clinical Trial
    分子量

    499.61

    Formula

    C28H33N7O2

    CAS 号
    性状

    固体

    颜色

    Light yellow to brown

    中文名称

    奥斯替尼;奥希替尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (200.16 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0016 mL 10.0078 mL 20.0156 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.00 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 方案 二

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.00 mM); 澄清溶液

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: 0.5%HPMC  1%Tween80

      Solubility: 5 mg/mL (10.01 mM); Suspened solution; 超声助溶 (<60°C)

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.96%

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0016 mL 10.0078 mL 20.0156 mL 50.0390 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 mL 10.0078 mL
    10 mM 0.2002 mL 1.0008 mL 2.0016 mL 5.0039 mL
    15 mM 0.1334 mL 0.6672 mL 1.3344 mL 3.3359 mL
    20 mM 0.1001 mL 0.5004 mL 1.0008 mL 2.5020 mL
    25 mM 0.0801 mL 0.4003 mL 0.8006 mL 2.0016 mL
    30 mM 0.0667 mL 0.3336 mL 0.6672 mL 1.6680 mL
    40 mM 0.0500 mL 0.2502 mL 0.5004 mL 1.2510 mL
    50 mM 0.0400 mL 0.2002 mL 0.4003 mL 1.0008 mL
    60 mM 0.0334 mL 0.1668 mL 0.3336 mL 0.8340 mL
    80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6255 mL
    100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5004 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Osimertinib
    目录号:
    HY-15772
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