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  2. Cell Cycle/DNA Damage
  3. Wee1
  4. Adavosertib

Adavosertib  (Synonyms: AZD1775; MK-1775)

目錄號: HY-10993 純度: 99.97%
COA 產(chǎn)品使用指南

Adavosertib (AZD-1775; MK-1775) 是一種有效的 Wee1 抑制劑，IC50 值為 5.2 nM。

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Adavosertib Chemical Structure

Adavosertib Chemical Structure

CAS No. : 955365-80-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥738
In-stock
1 mg ￥291
In-stock
5 mg ￥670
In-stock
10 mg ￥1079
In-stock
25 mg ￥1975
In-stock
50 mg ￥3113
In-stock
100 mg ￥4363
In-stock
200 mg 現(xiàn)貨 詢價
500 mg 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Adavosertib:

MCE 顧客使用本產(chǎn)品發(fā)表的 46 篇科研文獻

WB

    Adavosertib purchased from MCE. Usage Cited in: J Hematol Oncol. 2018 Aug 1;11(1):99.  [Abstract]

    Representative immunoblots showing the expression of key proteins of the WEE1 pathway after treatment with AZD-1775 (IC50 for each cell line) for 24 h of the indicated cells lines. β-actin is used for loading normalization.

    Adavosertib purchased from MCE. Usage Cited in: Cancer Res. 2017 Sep 1;77(17):4663-4672.  [Abstract]

    Isogenic A549 or H2030 cells expressing full-length LKB1 or kinase-dead LKB1(KDLKB1) are treated with 1 μM AZD1775 or vehicle (DMSO) for 24 hours. Protein lysates are immunoblotted with the indicated antibodies. Actin was used as a loading control.

    Adavosertib purchased from MCE. Usage Cited in: Scienze biomediche. University of Bologna. 2016 Apr.

    In the blots B-/T-ALL cell lines are incubated for 24 hours with MK-1775 (IC50 value). The homogeneity of the protein loaded (40 μg) is determined using an internal control (β-actin).

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.

    IC50 & Target

    IC50: 5.2 nM (Wee1)
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-427 IC50
    158 nM
    Compound: 1; AZD1775
    Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    		[PMID: 37197456]
    A-427 IC50
    78 nM
    Compound: AZD1775
    Antiproliferative activity against human A-427 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay
    Antiproliferative activity against human A-427 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay
    		[PMID: 34423975]
    BT-549 IC50
    0.49 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    Daoy IC50
    150 nM
    Compound: Adavosertib
    Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
    Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
    		[PMID: 33636537]
    HEK-293T IC50
    0.29 μM
    Compound: MK-1775
    Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay
    Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay
    		[PMID: 28792760]
    LNCaP IC50
    0.5 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    MCF7 IC50
    1.1 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    MDA-MB-231 IC50
    0.26 μM
    Compound: MK-1775
    Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay
    Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay
    		[PMID: 28792760]
    MM1.S IC50
    0.31 μM
    Compound: MK-1775
    Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay
    Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay
    		[PMID: 28792760]
    MV4-11 IC50
    95 nM
    Compound: AZD1775
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Celltiter-glo assay
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Celltiter-glo assay
    		[PMID: 37167712]
    NCI-H1299 IC50
    0.2837 nM
    Compound: AZD-1775; MK-1775
    Inhibition of cell proliferation in human NCI-H1299 cells incubated for 3 days by MTT assay
    Inhibition of cell proliferation in human NCI-H1299 cells incubated for 3 days by MTT assay
    		[PMID: 35051747]
    NCI-H1299 IC50
    104 nM
    Compound: AZD1775
    Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 3 days by CellTiter-Glo Luminescent assay
    Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 3 days by CellTiter-Glo Luminescent assay
    		[PMID: 36075370]
    NCI-H23 IC50
    122 nM
    Compound: AZD1775
    Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 4 days by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 4 days by CellTiter-Glo assay
    		[PMID: 34423975]
    NCI-H23 IC50
    175 nM
    Compound: 1; AZD1775
    Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay
    		[PMID: 37197456]
    PC-3 IC50
    8 μM
    Compound: 1; AZD1775
    Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay
    		[PMID: 35231578]
    T47D IC50
    12780 nM
    Compound: AZD1775
    Antiproliferative activity against human T47D cells incubated for 72 hrs by Celltiter-glo assay
    Antiproliferative activity against human T47D cells incubated for 72 hrs by Celltiter-glo assay
    		[PMID: 37167712]
    體外研究
    (In Vitro)

    Adavosertib (MK-1775) 增強 5-FU 在 p53 缺陷型人結(jié)腸癌細胞中的細胞毒性作用。Adavosertib (MK-1775) 抑制細胞中的 CDC2 Y15 磷酸化，消除由 5-FU 誘導的 DNA 損傷檢查點，并導致通過誘導組蛋白 H3 磷酸化確定的有絲分裂過早進入[1]。
    Adavosertib (MK-1775) 可消除 p53 缺陷細胞中輻射誘導的 G2 阻滯，但不會消除 p53 野生型細胞系[2]。
    在 p53 缺陷型腫瘤中，NSC 613327 與 Adavosertib (MK-1775) 的組合產(chǎn)生強大的抗腫瘤活性，并且與 NSC 613327 處理相比顯著增強腫瘤消退反應 (4.01 倍)[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    在體內(nèi)，Adavosertib (MK-1775) 在可耐受劑量下增強 5-FU 的抗腫瘤功效[1]。
    Adavosertib (MK-1775) (60 mg/kg，每天兩次，口服) 增強 H1299 異種移植腫瘤對分次放療的反應[2]。
    與 GEM 處理的小鼠相比，Adavosertib (MK-1775) (30 mg/kg，口服) 抑制 PANC198、PANC215 和 PANC185 的腫瘤生長[3]。

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

    500.60

    Formula

    C27H32N8O2
    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    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 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 125 mg/mL (249.70 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 1.9976 mL 9.9880 mL 19.9760 mL
    5 mM 0.3995 mL 1.9976 mL 3.9952 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，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.87 mg/mL (5.73 mM); 澄清溶液

    • 方案 二

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

      Solubility: ≥ 2.08 mg/mL (4.16 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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。

    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% Methylcellulose/saline water

      Solubility: 5 mg/mL (9.99 mM); Suspension solution; 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: 99.97%

    參考文獻
    Cell Assay
    [2]

    Total protein is extracted from the cell pellet using a lysis solution containing 50 mM HEPES (pH 7.9), 0.4 mol/L NaCl, and 1 mM EDTA and fortified with 10 μL/mL phosphatase inhibitor cocktail 1, 10 μL/mL phosphatase inhibitor cocktail 2, 10 μL/mL protease inhibitor, and 1% NP-40. Protein concentration of the lysates is determined by the Bio-Rad protein assay. Equal amounts of protein are separated by 12% SDS-PAGE and transferred to an Immobilon membrane. Nonspecific binding sites on the membrane are blocked in 5% nonfat dry milk in Tris (20 mM)-buffered saline (150 mM, pH 7.4) with 0.1% Tween (TBS-T). Protein signals are detected by incubating the membrane in primary antibody in 5% nonfat dry milk overnight at 4°C, followed by a 45-min incubation in the appropriate peroxidase-conjugated secondary antibody. The membrane is then developed by enhanced chemiluminescence with ECL plus Western Blotting Detection Reagents on a Typhoon 9400 scanner.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Tumor xenografts are produced in the leg by im inoculation of 1×106?Calu-6 cells in 10 μL. Irradiation and Adavosertib (MK-1775) treatment are started when tumors reach 8 mm diameter and continue for 5 days. Gamma-rays are delivered locally to the tumor-bearing legs of unanesthetized mice using a small-animal irradiator consisting of two parallel-opposed?137Cs sources, at a dose rate of 5 Gy/min. Tumors are irradiated twice daily separated by 6 h. Adavosertib (MK-1775) is given by gavage in 0.1 mL volumes 1 h before and 2 h after the first daily radiation dose.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6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 1.9976 mL 9.9880 mL 19.9760 mL 49.9401 mL
    5 mM 0.3995 mL 1.9976 mL 3.9952 mL 9.9880 mL
    10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9940 mL
    15 mM 0.1332 mL 0.6659 mL 1.3317 mL 3.3293 mL
    20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4970 mL
    25 mM 0.0799 mL 0.3995 mL 0.7990 mL 1.9976 mL
    30 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6647 mL
    40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
    50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
    60 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8323 mL
    80 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
    100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4994 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：
    Adavosertib
    目錄號：
    HY-10993
    需求量：