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

Alectinib Hydrochloride  (Synonyms: 艾樂替尼鹽酸鹽; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

目錄號: HY-13011A 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 是一種有效，選擇性和口服的 ALK 抑制劑，其 IC50 為 1.9 nM，Kd 值為 2.4 nM (以 ATP 競爭方式)，并且還抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分別為 1 nM 和 3.5 nM。Alectinib Hydrochloride 還具有有效的中樞神經(jīng)系統(tǒng) (CNS) 滲透能力。

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Alectinib Hydrochloride Chemical Structure

Alectinib Hydrochloride Chemical Structure

CAS No. : 1256589-74-8

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規(guī)格 價格 是否有貨 數(shù)量
2 mg ￥291
In-stock
5 mg ￥460
In-stock
10 mg ￥646
In-stock
25 mg ￥1160
In-stock
50 mg ￥1500
In-stock
100 mg ￥1920
In-stock
200 mg ￥2495
In-stock
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Alectinib Hydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 34 篇科研文獻

WB

    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]

    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 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.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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]
    體外研究
    (In Vitro)

    Alectinib (0-1000 nM；2 小時；NCI-H2228 細胞) 處理可以防止表達 EML4-ALK 的 NCI-H2228 細胞中 ALK 的自磷酸化，并且還可以顯著抑制 STAT3 和 AKT 的磷酸化[1]。
    Alectinib (0-1000 nM；5 天；HCC827、A549 或 NCIH522 細胞) 處理以劑量依賴性方式降低細胞活性[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.
    體內(nèi)研究
    (In Vivo)

    Alectinib Hydrochloride (0.2 -20 mg/kg；口服給藥；每日一次；持續(xù) 11 天；SCID 或攜帶 NCI-H2228 細胞的裸鼠) 處理可導致劑量依賴性腫瘤生長抑制 (EC50 0.46 mg/kg) 和腫瘤消退。在任何劑量水平下，均未觀察到體重差異或總體毒性跡象[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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    艾樂替尼鹽酸鹽；鹽酸阿雷替尼
    運輸條件

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

    4°C, sealed storage, away from moisture

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

    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 2 mg/mL (3.85 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9265 mL 9.6324 mL 19.2649 mL
    5 mM --- --- ---
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.92%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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    產(chǎn)品名稱：
    Alectinib Hydrochloride
    目錄號：
    HY-13011A
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