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

Neratinib  (Synonyms: 來那替尼; HKI-272)

目錄號: HY-32721 純度: 99.94%
COA 產(chǎn)品使用指南

Neratinib (HKI-272) 是一種具有口服活性的、不可逆的、高選擇性的 HER2 和 EGFR 抑制劑，IC50 值分別為 59 nM 和 92 nM。

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Neratinib Chemical Structure

Neratinib Chemical Structure

CAS No. : 698387-09-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
In-stock
5 mg ￥350
In-stock
10 mg ￥600
In-stock
25 mg ￥950
In-stock
50 mg ￥1300
In-stock
100 mg ￥2300
In-stock
200 mg ￥4200
In-stock
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Neratinib:

    Neratinib purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jun 20;10(446):eaao2565.  [Abstract]

    Immunoblots of 3 individual KM tumors from mice treated for 3 days with Neratinib or vehicle control.

    Neratinib purchased from MCE. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176.  [Abstract]

    Influence of BIBW 2992 or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively[1].

    IC50 & Target[1]

    HER2

    59 nM (IC50)

    EGFR

    92 nM (IC50)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BaF3 GI50
    1.9 μM
    Compound: 2; HKI272
    Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 28282122]
    BT-474 IC50
    2.06 nM
    Compound: Neratinib
    Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    COLO-678 IC50
    694.11 nM
    Compound: Neratinib
    Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    ES-2 IC50
    787.91 nM
    Compound: Neratinib
    Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    MDA-MB-468 IC50
    405.51 nM
    Compound: Neratinib
    Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    MFE-280 IC50
    1291.95 nM
    Compound: Neratinib
    Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    NCI-H441 IC50
    1280.72 nM
    Compound: Neratinib
    Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    NCI-N87 IC50
    0.64 nM
    Compound: Neratinib
    Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    NUGC-4 IC50
    38.15 nM
    Compound: Neratinib
    Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    Sf9 IC50
    2.5 nM
    Compound: 3, HKI-272
    Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
    Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
    		[PMID: 24900643]
    Sf9 IC50
    66 nM
    Compound: 3, HKI-272
    Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
    Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
    		[PMID: 24900643]
    SK-BR-3 IC50
    10.34 nM
    Compound: Neratinib
    Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 35319895]
    SK-BR-3 IC50
    7.2 nM
    Compound: 45
    Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by sulforhodamine B colorimetric assay
    Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by sulforhodamine B colorimetric assay
    		[PMID: 36332549]
    體外研究
    (In Vitro)

    Neratinib 對其他絲氨酸-蘇氨酸激酶沒有活性，例如 Akt、細胞周期蛋白 D1/cdk4、細胞周期蛋白 E/cdk2、細胞周期蛋白 B1/cdk1、IKK-2、MK-2、PDK1、c-Raf 和 Tpl-2，以及作為酪氨酸激酶 c-Met[1]。
    Neratinib (0.5 ng/mL–5 μg/mL，2 天) 抑制顯示高水平 HER-2 (3T3/neu、SK-Br-3 和 BT474) 并且在既不表達 HER-2 也不表達 EGFR (3T3、MDA-MB-435 和 SW620) 的細胞系中活性低得多[1]。
    Neratinib (0-2 nM，12-16 小時) 將 BT474 細胞周期停滯在 G1-S 期[1]。
    Neratinib 抑制 MAPK 和 Akt 磷酸化、細胞周期蛋白 D1 水平的下調(diào)和 p27[1]的誘導(dǎo)。

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

    Cell Proliferation Assay[1]

    Cell Line: 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620
    Concentration: 0.5 ng/mL–5 μg/mL
    Incubation Time: 2 days (6 days for BT474)
    Result: Inhibited cell proliferation with IC50 values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.

    Western Blot Analysis[1]

    Cell Line: BT474 or A431 cells
    Concentration: 0, 2, 10, 50, 100 and 200 nM
    Incubation Time: 3 h
    Result: Decreased ligand-independent receptor phosphorylation by 50% (IC50) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC50 = 3 nM).
    Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.

    Cell Cycle Analysis[1]

    Cell Line: BT474
    Concentration: 0–2 nM
    Incubation Time: 12–16 h
    Result: Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.
    體內(nèi)研究
    (In Vivo)

    Neratinib (HKI-272) (0 -80 mg/kg/天；ig；42 天) 對表達高水平 HER-2 或 EGFR 的癌細胞顯示出抗癌活性[1]。

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

    Animal Model: Female athymic (nude) mice, tumor xenograft[1]
    Dosage: 10, 20, 40, 60 or 80 mg/kg/day
    Administration: Gavage, 42 days
    Result: Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.
    Clinical Trial
    分子量

    557.04

    Formula

    C30H29ClN6O3
    CAS 號
    性狀

    固體

    顏色

    White to light brown

    中文名稱

    來那替尼
    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 : 13.33 mg/mL (23.93 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)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.7952 mL 8.9760 mL 17.9520 mL
    5 mM 0.3590 mL 1.7952 mL 3.5904 mL
    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(fù)凍融造成的產(chǎn)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(nèi)使用， -20°C儲存時，請在1年內(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(jié)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(nèi)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    90% (20% SBE-β-CD in Saline)

      Solubility: 2 mg/mL (3.59 mM); 懸濁液; 超聲助溶

      此方案可獲得 2 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    • 方案 二

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

      Solubility: ≥ 0.83 mg/mL (1.49 mM); 澄清溶液

      此方案可獲得 ≥ 0.83 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 8.3 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。

    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(nèi)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% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 3.33 mg/mL (5.98 mM); 懸濁液; 超聲助溶

    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
    請輸入您的動物體內(nèi)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， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.94%

    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(fù)凍融造成的產(chǎn)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(nèi)使用， -20°C儲存時，請在1年內(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 1.7952 mL 8.9760 mL 17.9520 mL 44.8801 mL
    5 mM 0.3590 mL 1.7952 mL 3.5904 mL 8.9760 mL
    10 mM 0.1795 mL 0.8976 mL 1.7952 mL 4.4880 mL
    15 mM 0.1197 mL 0.5984 mL 1.1968 mL 2.9920 mL
    20 mM 0.0898 mL 0.4488 mL 0.8976 mL 2.2440 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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    產(chǎn)品名稱：
    Neratinib
    目錄號：
    HY-32721
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