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

Alectinib  (Synonyms: 艾乐替尼; CH5424802; RO5424802; RG7853)

目录号: HY-13011 纯度: 99.78%
COA 产品使用指南 技术支持

Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 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 还具有有效的中枢神经系统 (CNS) 渗透能力。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Alectinib Chemical Structure

Alectinib Chemical Structure

CAS No. : 1256580-46-7

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Customer Review

Other Forms of Alectinib:

MCE 顾客使用本产品发表的 34 篇科研文献

WB

    Alectinib 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 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.

    Alectinib 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.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Alectinib (CH5424802) 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]

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BaF3 IC50
    > 1000 nM
    Compound: 1
    Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    169 nM
    Compound: 1
    Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    2 nM
    Compound: 1
    Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    2 nM
    Compound: 1
    Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    2 nM
    Compound: 1
    Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    207 nM
    Compound: 1
    Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    3 nM
    Compound: 1
    Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    72 nM
    Compound: 1
    Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    9 nM
    Compound: 1
    Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    BaF3 IC50
    90 nM
    Compound: 1
    Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 26568289]
    KARPAS-299 IC50
    15 nM
    Compound: 3; CH5424802
    Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    KARPAS-299 IC50
    3 nM
    Compound: Alectinib
    Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay
    [PMID: 34402300]
    KARPAS-299 IC50
    3 nM
    Compound: 18a, CH5424802
    Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay
    Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay
    [PMID: 22225917]
    KARPAS-299 IC50
    47 nM
    Compound: 3
    Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 34176264]
    Kelly EC50
    434 nM
    Compound: 1
    Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    NB1 IC50
    4.5 nM
    Compound: Alectinib
    Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay
    [PMID: 34402300]
    NCI-H2228 IC50
    53 nM
    Compound: Alectinib
    Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay
    [PMID: 34402300]
    NCI-H2228 IC50
    6.5 nM
    Compound: CH5424802
    Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
    Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay
    [PMID: 31425908]
    NCI-H3122 IC50
    17.4 nM
    Compound: 3; CH5424802
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    NCI-H3122 IC50
    19 nM
    Compound: 5
    Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
    Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
    [PMID: 26476749]
    NCI-H3122 IC50
    45 nM
    Compound: 3
    Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against ALK-positive human NCI-H3122 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 34176264]
    NCI-H3122 EC50
    9 nM
    Compound: 1
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    NIH3T3 IC50
    132 nM
    Compound: 3; CH5424802
    Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    NIH3T3 IC50
    32.3 nM
    Compound: 3; CH5424802
    Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    SH-SY5Y EC50
    1150 nM
    Compound: 1
    Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SK-N-AS EC50
    2139 nM
    Compound: 1
    Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SK-N-FI EC50
    2401 nM
    Compound: 1
    Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SK-N-SH EC50
    872 nM
    Compound: 1
    Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
    [PMID: 26568289]
    SU-DHL-1 IC50
    20.5 nM
    Compound: 3; CH5424802
    Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay
    Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay
    [PMID: 27131066]
    体外研究
    (In Vitro)

    Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
    Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[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 (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[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

    482.62

    Formula

    C30H34N4O2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    艾乐替尼;阿雷替尼

    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
    细胞实验: 

    DMSO 中的溶解度 : 4.33 mg/mL (8.97 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 2.0720 mL 10.3601 mL 20.7202 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 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

    动物实验:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.38 mg/mL (0.79 mM); 澄清溶液

      此方案可获得 ≥ 0.38 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 3.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 0.38 mg/mL (0.79 mM); 澄清溶液

      此方案可获得 ≥ 0.38 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 3.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    以下溶解方案,请直接配制工作液。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% CMC-Na/saline water

      Solubility: 12.5 mg/mL (25.90 mM); 悬浊液; 超声助溶

    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: 99.78%

    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 2.0720 mL 10.3601 mL 20.7202 mL 51.8006 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 mL 10.3601 mL
    Help & FAQs
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      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:
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    目录号:
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