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

Alectinib  (Synonyms: 艾樂替尼; CH5424802; RO5424802; RG7853)

目錄號: HY-13011 純度: 99.78%
COA 產品使用指南

Alectinib (CH5424802) 是一種有效、選擇性、具有口服活性的 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 F1174LALK R1275Q,其 IC50 分別為 1 nM 和 3.5 nM。Alectinib 還具有有效的中樞神經系統(tǒng) (CNS) 滲透能力。

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Alectinib Chemical Structure

Alectinib Chemical Structure

CAS No. : 1256580-46-7

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Customer Review

Other Forms of Alectinib:

MCE 顧客使用本產品發(fā)表的 34 篇科研文獻

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

    • 純度 & 產品資料

    • 參考文獻

    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]

    細胞效力
    (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]
    體外研究
    (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.
    體內研究
    (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 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    艾樂替尼;阿雷替尼

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 4.33 mg/mL (8.97 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質量 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
    查看完整儲備液配制表

    * 請根據(jù)產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品失效。
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內使用, -20°C儲存時,請在1年內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 0.38 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 3.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% Corn Oil

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

      此方案可獲得 ≥ 0.38 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

      1 mL 工作液為例,取 100 μL 3.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: 0.5% CMC-Na/saline water

      Solubility: 12.5 mg/mL (25.90 mM); 懸濁液; 超聲助溶

    掃碼獲得
    動物溶解方案

    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

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, PEG300/PEG400,Tween 80,均可在 MCE 網(wǎng)站選購。
    純度 & 產品資料

    純度: 99.78%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產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品失效
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內使用, -20°C儲存時,請在1年內使用。

    可選溶劑 濃度 溶劑體積 質量 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

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    目錄號:
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