1. Protein Tyrosine Kinase/RTK
  2. Anaplastic lymphoma kinase (ALK)
  3. Alectinib Hydrochloride

Alectinib Hydrochloride  (Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

目录号: HY-13011A 纯度: 99.93%
COA 产品使用指南

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 是一种有效,选择性和口服的 ALK 抑制剂,其 IC50 为 1.9 nM,Kd 值为 2.4 nM (以 ATP 竞争方式),并且还抑制 ALK F1174LALK R1275Q,其 IC50 分别为 1 nM 和 3.5 nM。Alectinib Hydrochloride 还具有有效的中枢神经系统 (CNS) 渗透能力。

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Alectinib Hydrochloride Chemical Structure

Alectinib Hydrochloride Chemical Structure

CAS No. : 1256589-74-8

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Top Publications Citing Use of Products

    Alectinib Hydrochloride purchased from MCE. Usage Cited in: Cell Death Discov. 2018 May 10;4:56.  [Abstract]

    NB39-nu cells are treated with either 1000 nM Crizotinib (CR) or Alectinib (AL) for the indicated times and subjected to immunoblot analysis. CLTC is the loading control.

    Alectinib Hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 1;400:61-68.  [Abstract]

    Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells are treated with 10 mM alectinib for various time points as indicated. The anti-b-Actin antibody is used as a loading control for whole cell extracts.

    Alectinib Hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 1;400:61-68.  [Abstract]

    In contrast to tumors treated with DMSO, tumors treated with Alectinib exhibits significantly decreased levels of p-Akt and p-S6. Furthermore, increased PARP and Caspase 3 cleavages are observed in tumors treated with Alectinib compared to controls.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

    IC50 & Target

    IC50: 1.9 nM (ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
    Kd: 2.4 nM (ALK)[1]

    体外研究
    (In Vitro)

    Alectinib (0-1000 nM;2 小时;NCI-H2228 细胞) 处理可以防止表达 EML4-ALK 的 NCI-H2228 细胞中 ALK 的自磷酸化,并且还可以显著抑制 STAT3AKT 的磷酸化[1]
    Alectinib (0-1000 nM;5 天;HCC827、A549 或 NCIH522 细胞) 处理以剂量依赖性方式降低细胞活性[1]

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

    Western Blot Analysis[1]

    Cell Line: NCI-H2228 cells
    Concentration: 0 nM,10 nM,100 nM, 1000 nM
    Incubation Time: 2 hours
    Result: Inhibition of ALK phosphorylation and signal transduction.

    Cell Viability Assay[1]

    Cell Line: HCC827, A549, or NCIH522 cells
    Concentration: 0-1000 nM
    Incubation Time: 5 days
    Result: Reduced cell activity in a dose-dependent manner.
    体内研究
    (In Vivo)

    Alectinib Hydrochloride (0.2 -20 mg/kg;口服给药;每日一次;持续 11 天;SCID 或携带 NCI-H2228 细胞的裸鼠) 处理可导致剂量依赖性肿瘤生长抑制 (EC50 0.46 mg/kg) 和肿瘤消退。在任何剂量水平下,均未观察到体重差异或总体毒性迹象[1]

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

    Animal Model: SCID or nude mice bearing NCI-H2228 cells[1]
    Dosage: 0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
    Administration: Oral administration; once daily; for 11 days
    Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.
    Clinical Trial
    分子量

    519.08

    Formula

    C30H35ClN4O2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    艾乐替尼盐酸盐;盐酸阿雷替尼

    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
    In Vitro: 

    DMSO 中的溶解度 : 2 mg/mL (3.85 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9265 mL 9.6324 mL 19.2649 mL
    5 mM --- --- ---
    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。

    • 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

    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
    纯度 & 产品资料

    纯度: 99.93%

    参考文献

    Alectinib Hydrochloride 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 1 mM 1.9265 mL 9.6324 mL 19.2649 mL 48.1621 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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    Alectinib Hydrochloride
    目录号:
    HY-13011A
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