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  2. Cell Cycle/DNA Damage Apoptosis
  3. Polo-like Kinase (PLK) Apoptosis
  4. Volasertib

Volasertib  (Synonyms: 伏拉塞替; BI 6727)

目錄號: HY-12137 純度: 99.41%
COA 產(chǎn)品使用指南

Volasertib (BI 6727) 是一種具有口服活性的、高效的、ATP 競爭性的 Polo 樣激酶 1 (PLK1) 抑制劑，IC50 為 0.87 nM。Volasertib 抑制 PLK2 和 PLK3，IC50 分別為 5 和 56 nM。Volasertib 誘導(dǎo)有絲分裂停滯和細(xì)胞凋亡。Volasertib 是一種二氫蝶呤酮衍生物，在多種癌癥模型中顯示出顯著的抗腫瘤活性。

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Volasertib Chemical Structure

Volasertib Chemical Structure

CAS No. : 755038-65-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1116
In-stock
1 mg ￥340
In-stock
5 mg ￥820
In-stock
10 mg ￥1300
In-stock
25 mg ￥2725
In-stock
50 mg ￥3750
In-stock
100 mg ￥5200
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Volasertib:

    Volasertib purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;43(4):1472-1486.  [Abstract]

    The addition of Volasertib (0.5-1.5 μg/mL blunts the increase of the percentage of annexin-V-binding erythrocytes following glucose deprivation, an effect reaching statistical significance at 1 and 1.5 μg/mL Volasertib.

    查看 Polo-like Kinase (PLK) 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2].

    IC50 & Target[3]

    PLK1

    0.87 nM (IC50)

    PLK2

    5 nM (IC50)

    PLK3

    56 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    4137 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    A-427 IC50
    91 nM
    Compound: 44
    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]
    A549 IC50
    0.08 μM
    Compound: BI6727; I
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 30572179]
    A549 IC50
    206.4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    DU-145 IC50
    < 4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    HCT-116 IC50
    0.11 μM
    Compound: BI6727; I
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 30572179]
    HCT-116 IC50
    602.4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    HEK-293T IC50
    1.1 nM
    Compound: Volasertib
    Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
    Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
    		[PMID: 34710325]
    HepG2 IC50
    < 4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    HT-29 IC50
    1133 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    JeKo-1 IC50
    < 4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    K562 IC50
    < 4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    KARPAS-299 IC50
    < 4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    L02 IC50
    < 4 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    MCF7 IC50
    0.09 μM
    Compound: BI6727; I
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 30572179]
    MDA-MB-231 IC50
    0.11 μM
    Compound: BI6727; I
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 30572179]
    MDA-MB-231 IC50
    1482 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    MM1.S IC50
    4.5 nM
    Compound: Volasertib
    Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
    Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
    		[PMID: 34710325]
    NCI-H23 IC50
    53 nM
    Compound: 44
    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
    0.09 μM
    Compound: BI6727; I
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 30572179]
    SMMC-7721 IC50
    77.2 nM
    Compound: 3; BI 6727
    Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
    		[PMID: 32814244]
    體外研究
    (In Vitro)

    Volasertib (BI 6727；0.01-10000 nM；72 小時) 在多種細(xì)胞系[1]中的 EC50 值為 11 至 37 nmol/L。
    Volasertib (10-1000 nM；24 小時) 導(dǎo)致細(xì)胞積累 4N DNA 含量，表明細(xì)胞周期阻滯在 G2-M 期[1]。
    Volasertib (100 nM；24-72 hours) 在 48 小時誘導(dǎo)細(xì)胞凋亡[1]。

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

    Cell Proliferation Assay[1]

    Cell Line: Multiple cell lines
    Concentration: 0.01-10000 nM
    Incubation Time: 72 hours
    Result: Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC50=23 nmol/L) and lung (NCI-H460, EC50=21 nmol/L), melanoma (BRO, EC50=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC50=15 nmol/L; HL-60, EC50=32 nmol/L; THP-1, E50=36 nmol/L and Raji, EC50=37 nmol/L) with EC50 values of 11 to 37 nmol/L.

    Apoptosis Analysis[1]

    Cell Line: NCI-H460 cells
    Concentration: 100 nM
    Incubation Time: 24, 48, 72 hours
    Result: G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours.

    Cell Cycle Analysis[1]

    Cell Line: NCI-H460 cells
    Concentration: 10, 30, 100, 300, 1000 nM
    Incubation Time: 24 hours
    Result: Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.
    體內(nèi)研究
    (In Vivo)

    Volasertib (BI 6727；每周總劑量為 50 mg/kg；口服；每周一次、每周兩次或每天一次；持續(xù) 40 天) 在人結(jié)腸癌異種移植模型中顯示出相當(dāng)?shù)寞熜?sup>[1]。
    Volasertib (15、20 或 25 mg/kg/天；靜脈注射；每周連續(xù) 2 天；持續(xù) 40 天) 在人結(jié)腸癌異種移植模型中導(dǎo)致顯著的腫瘤生長延遲甚至腫瘤消退[1]。
    Volasertib (70 mg/kg，每周一次或每天 10 mg/kg；口服) 顯著延遲源自 NCI-H460 細(xì)胞的非小細(xì)胞肺癌異種移植模型中的腫瘤生長[1]。
    Volasertib (單劑量 40 mg/kg；靜脈注射) 導(dǎo)致 HCT 116 荷瘤裸鼠的有絲分裂細(xì)胞顯著增加 (13 倍)[1]。
    Volasertib 在小鼠體內(nèi)分布容積大，終末半衰期長 (Vss=7.6 L/kg，t1/2=46 h) 和大鼠 (Vss=22 L/kg，t1/2=54 h)[1]。

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

    Animal Model: Female BomTac:NMRI-Foxn1nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)[1]
    Dosage: A total weekly dose of 50 mg/kg
    Administration: Oral; once a week, twice a week, or daily; for 40 days
    Result: Showed comparable efficacy and were well tolerated.
    Animal Model: Female BomTac:NMRI-Foxn1nu mice and male Wistar rats of the strain Crl:WI[1]
    Dosage: 35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis)
    Administration: IV 5-minute infusion; a single dose 5-minute infusion
    Result: Had high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h).
    Clinical Trial
    分子量

    618.81

    Formula

    C34H50N8O3
    CAS 號
    性狀

    固體

    顏色

    Off-white to light yellow

    中文名稱

    伏拉塞替
    運輸條件

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

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : 25 mg/mL (40.40 mM; 超聲助溶 (<60°C); 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 1.6160 mL 8.0800 mL 16.1600 mL
    5 mM 0.3232 mL 1.6160 mL 3.2320 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, 6 months; -20°C, 1 month (protect from light)。-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

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?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(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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: ≥ 2.08 mg/mL (3.36 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。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (3.36 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 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 20.8 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。
    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）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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(jǐn)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: 99.41%

    參考文獻(xiàn)

    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, 6 months; -20°C, 1 month (protect from light)。-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 1.6160 mL 8.0800 mL 16.1600 mL 40.4001 mL
    5 mM 0.3232 mL 1.6160 mL 3.2320 mL 8.0800 mL
    10 mM 0.1616 mL 0.8080 mL 1.6160 mL 4.0400 mL
    15 mM 0.1077 mL 0.5387 mL 1.0773 mL 2.6933 mL
    20 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0200 mL
    25 mM 0.0646 mL 0.3232 mL 0.6464 mL 1.6160 mL
    30 mM 0.0539 mL 0.2693 mL 0.5387 mL 1.3467 mL
    40 mM 0.0404 mL 0.2020 mL 0.4040 mL 1.0100 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：
    Volasertib
    目錄號：
    HY-12137
    需求量：