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

Osimertinib dimesylate  (Synonyms: 奥希替尼二甲磺酸盐; AZD-9291 dimesylate; Mereletinib dimesylate)

目录号: HY-79077 纯度: 99.19%
COA 产品使用指南

摩尔计算器

Osimertinib dimesylate (AZD-9291 dimesylate) 是不可逆的突变体选择性 EGFR 抑制剂；对EGFRL858R 和EGFRL858R/T790M 的 IC50 值分别为12 和 1 nM。

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Osimertinib dimesylate Chemical Structure

Osimertinib dimesylate Chemical Structure

CAS No. : 2070014-82-1

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥761
In-stock
5 mg ￥500
In-stock
10 mg ￥700
In-stock
50 mg ￥1400
In-stock
100 mg ￥1900
In-stock
200 mg ￥2800
In-stock
500 mg ￥5000
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Osimertinib dimesylate:

Osimertinib dimesylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 107 篇科研文献

Proliferation Assay
WB

    Osimertinib dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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.

    查看 EGFR 亚型特异性产品:

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    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50)

    EGFRL858R/T790M

    1 nM (IC50)

    体外研究
    (In Vitro)

    Osimertinib (AZD-9291) 在抑制含有敏感 EGFR 突变体 (包括 PC-9 (ex19del)、H3255 (L858R) 和 H1650 (ex19del) ) 的 EGFR 细胞中的 EGFR 磷酸化方面显示出与早期酪氨酸激酶抑制剂 (TKI) 相似的效力，平均 IC奥希替尼 (AZD-9291) 的 50 值范围为 13 至 54 nM。Osimertinib (AZD-9291) 还有效抑制 T790M 突变细胞系 (H1975 (L858R/T790M)、PC-9VanR (ex19del/T790M) 中 EGFR 的磷酸化，平均 IC50 效力小于 15 nM[1]。

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

    Osimertinib dimesylate 相关抗体:
    体内研究
    (In Vivo)

    荷瘤小鼠用 Osimertinib (AZD-9291)? (5 mg/kg/天) 处理一到两周。在处理的几天内，5 只 C/L858R 小鼠中有 5 只在Osimertinib (AZD-9291) 处理后通过磁共振成像 MRI 显示肿瘤体积缩小了近 80%，而用载体处理的 5 只小鼠中有 5 只显示肿瘤生长[1]。
    与之前描述的化合物相比，奥希替尼 (AZD-9291) 显示大鼠 PK 得到改善，hERG 亲和力降低，IGF1R 边缘得到改善，因此选择该化合物进行进一步研究。与之前描述的先导化合物相比，Osimertinib (AZD-9291) 还提供了更广泛的化学和特征多样性。在三种功效模型中给予 Osimertinib (AZD-9291) 后，在相对较低的剂量 (每天 10 mg/kg) 下观察到可比较的功效。当 Osimertinib (AZD-9291) 以每天 5 mg/kg 的剂量给药时，也观察到了出色的疗效[2]。

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

    691.82

    Formula

    C30H41N7O8S2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    奥斯替尼二甲磺酸盐；奥希替尼二甲磺酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 100 mg/mL (144.55 mM; 超声助溶)

    DMSO 中的溶解度 : 2.63 mg/mL (3.80 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 1.4455 mL 7.2273 mL 14.4546 mL
    5 mM 0.2891 mL 1.4455 mL 2.8909 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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

    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

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.96%

    COA (273 KB) HNMR (177 KB) LCMS (401 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM ZD1839, 1.5 μM BIBW 2992, 1.5 μM WZ4002 or 160 nM Osimertinib (AZD-9291) are achieved[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Mice[1]
    The EGFRL858R and EGFRL858R+T790M mice (male and female) are used. Osimertinib (AZD-9291) is suspended in 1% Polysorbate 80 and administered via oral gavage once daily at the doses of 7.5 mg/kg and 5 mg/kg, respectively. Mice are imaged weekly at the Vanderbilt University Institute of Imaging Science. For immunoblot analysis, mice are treated for eight hours with drug as described before dissection and flash freezing of the lungs. Lungs are pulverized in liquid nitrogen before lysis.
    Rats[2]
    The male RccHan:WIST rats (10-week-old) are received a single oral dose of Osimertinib (AZD-9291) (200 mg/kg). Blood glucose levels are measured using an Accuchek Active meter.

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

    Osimertinib dimesylate 相关分类

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.4455 mL 7.2273 mL 14.4546 mL 36.1366 mL
    H2O 5 mM 0.2891 mL 1.4455 mL 2.8909 mL 7.2273 mL
    10 mM 0.1445 mL 0.7227 mL 1.4455 mL 3.6137 mL
    15 mM 0.0964 mL 0.4818 mL 0.9636 mL 2.4091 mL
    20 mM 0.0723 mL 0.3614 mL 0.7227 mL 1.8068 mL
    25 mM 0.0578 mL 0.2891 mL 0.5782 mL 1.4455 mL
    30 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2046 mL
    40 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.9034 mL
    50 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 mL
    60 mM 0.0241 mL 0.1205 mL 0.2409 mL 0.6023 mL
    80 mM 0.0181 mL 0.0903 mL 0.1807 mL 0.4517 mL
    100 mM 0.0145 mL 0.0723 mL 0.1445 mL 0.3614 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    Keywords:

    Osimertinib dimesylate2070014-82-1AZD-9291 dimesylateMereletinib dimesylate奥斯替尼二甲磺酸盐奥希替尼二甲磺酸盐EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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