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  2. Protein Tyrosine Kinase/RTK
  3. FAK
  4. Defactinib

Defactinib  (Synonyms: VS-6063; PF-04554878)

目錄號(hào): HY-12289 純度: 99.87%
COA 產(chǎn)品使用指南 技術(shù)支持

Defactinib (VS-6063; PF-04554878) 是一種新型 FAK 抑制劑，抑制 FAK 在 Tyr397 位點(diǎn)磷酸化，這種作用具有時(shí)間和劑量依賴性。

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Defactinib Chemical Structure

Defactinib Chemical Structure

CAS No. : 1073154-85-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥898
In-stock
5 mg ￥800
In-stock
10 mg ￥1200
In-stock
50 mg ￥3000
In-stock
100 mg ￥4200
In-stock
200 mg 現(xiàn)貨 詢價(jià)
500 mg   詢價(jià)  
1 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Defactinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 38 篇科研文獻(xiàn)

WB

    Defactinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jul 28;37(1):175.  [Abstract]

    Western blot verified the inhibition of FAK Y397 phosphorylation via Defactinib in MCF7-YAP-S127A and MDA-MB-231 cells.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

    IC50 & Target

    FAK[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A375P GI50
    5.94 μM
    Compound: VS-6063; PF-04554878
    Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
    		[PMID: 34324343]
    A549 IC50
    4.09 μM
    Compound: 7
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    BXPC-3 IC50
    3.25 μM
    Compound: 7
    Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    HCT-116 IC50
    2.65 μM
    Compound: 5; VS-6063
    Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    		[PMID: 31129452]
    HCT-116 GI50
    9.13 μM
    Compound: VS-6063; PF-04554878
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
    		[PMID: 34324343]
    HCT-15 IC50
    4.36 μM
    Compound: 7
    Antiproliferative activity against human HCT-15 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-15 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    HEK293 IC50
    4.07 μM
    Compound: 7
    Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    HepG2 IC50
    3.69 μM
    Compound: 7
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    HUVEC IC50
    3.24 μM
    Compound: 7
    Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    L02 IC50
    4.66 μM
    Compound: 7
    Antiproliferative activity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    MCF-10A IC50
    18.42 μM
    Compound: 5; VS-6063
    Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay
    		[PMID: 31129452]
    MCF7 IC50
    5.81 μM
    Compound: 7
    Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    MCF7 IC50
    8.97 μM
    Compound: 5; VS-6063
    Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    		[PMID: 31129452]
    MDA-MB-231 GI50
    11.45 μM
    Compound: VS-6063; PF-04554878
    Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
    		[PMID: 34324343]
    MDA-MB-231 IC50
    3.75 μM
    Compound: 7
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    PANC-1 IC50
    3.48 μM
    Compound: 7
    Antiproliferative activity against human PANC-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human PANC-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 34091209]
    PC-3 IC50
    > 20 μM
    Compound: 5; VS-6063
    Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    		[PMID: 31129452]
    U-87MG ATCC IC50
    10.21 μM
    Compound: 5; VS-6063
    Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay
    		[PMID: 31129452]
    體外研究
    (In Vitro)

    Defactinib (VS-6063) 以時(shí)間和劑量依賴性方式抑制 Tyr397 位點(diǎn)的 FAK 磷酸化。RPPA 數(shù)據(jù)顯示，Defactinib 可降低紫杉烷耐藥細(xì)胞系中 AKT 和 YB-1 的水平。在所有細(xì)胞系中，pFAK (Tyr397) 的表達(dá)在統(tǒng)計(jì)學(xué)上被 Defactinib 以劑量依賴性方式顯著抑制。Defactinib 在 3 小時(shí)內(nèi)抑制 pFAK (Tyr397) 表達(dá)，并在 48 小時(shí)內(nèi)逐漸恢復(fù)表達(dá)[1]。

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

    Defactinib (VS-6063) 劑量為 25 mg/kg，每天兩次或更大，在 3 小時(shí)內(nèi)在統(tǒng)計(jì)學(xué)上顯著抑制 pFAK (Tyr397)，并在 24 小時(shí)內(nèi)恢復(fù)表達(dá)。因此，選擇以 25 mg/kg 每天兩次給藥 Defactinib 作為后續(xù)處理實(shí)驗(yàn)的給藥方案。對(duì)于處理實(shí)驗(yàn)，將腹腔內(nèi)攜帶 HeyA8 腫瘤的雌性裸鼠隨機(jī)分為 4 組 (每組 n=10)：1) 每天兩次口服載體，每周腹膜內(nèi)注射磷酸鹽緩沖鹽水 (對(duì)照)；2) Defactinib 25 mg/kg 口服，每天兩次；3) PTX 每周腹腔注射；和 4) 每天兩次口服 VDefactinib 25 mg/kg 和每周腹膜內(nèi)注射 PTX。在 HeyA8 模型中，PTX 單一療法使腫瘤重量減少了 87.4%，而聯(lián)合療法使腫瘤重量減少最多，減少了 97.9% (與 PTX 相比 P=0.05)。在 SKOV3ip1 模型中，與 PTX 相比，聯(lián)合處理組的腫瘤重量減輕了 92.7% (P<0.001)[1]。

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

    510.49

    Formula

    C20H21F3N8O3S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 50 mg/mL (97.95 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

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

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9589 mL 9.7945 mL 19.5890 mL
    5 mM 0.3918 mL 1.9589 mL 3.9178 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑： 2% DMSO    40% PEG300    5% Tween-80    53% Saline

      Solubility: 2.5 mg/mL (4.90 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.5 mg/mL (4.90 mM); 懸濁液; 超聲助溶

    以下溶解方案，請(qǐng)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(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (9.79 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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: 99.87%

    參考文獻(xiàn)
    Animal Administration
    [1]

    Mice[1]
    To determine the antitumor effects of Defactinib, SKOV3ip1, SKOV3-TR, HeyA8, and HeyA8-MDR cells are injected intraperitoneally. One week after tumor cell injection, mice are randomly assigned to 4 groups of 10 mice (control, PTX alone, Defactinib alone, and PTX with Defactinib); treatment is initiated at 3-4 weeks following injection. PTX at 2 mg/kg (SKOV3ip1 and SKOV3-TR) or 2.5 mg/kg (HeyA8 and HeyA8-MDR) is given intraperitoneally weekly; Defactinib at 25 mg/kg is given orally twice every day. Control mice received HBSS intraperitoneally once a week and vehicle orally twice every day. Mice are monitored daily for adverse effects of therapy and are killed on day 35 (SKOV3ip1 or SKOV3-TR), day 28 (HeyA8 or HeyA8-MDR), or when any of the mice seemed moribund. Total body weight, tumor incidence and mass, and the number of tumor nodules are recorded. Tumors are either fixed in formalin or embedded in paraffin or snap frozen in optimal cutting temperature (OCT) compound in liquid nitrogen.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)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 1.9589 mL 9.7945 mL 19.5890 mL 48.9726 mL
    5 mM 0.3918 mL 1.9589 mL 3.9178 mL 9.7945 mL
    10 mM 0.1959 mL 0.9795 mL 1.9589 mL 4.8973 mL
    15 mM 0.1306 mL 0.6530 mL 1.3059 mL 3.2648 mL
    20 mM 0.0979 mL 0.4897 mL 0.9795 mL 2.4486 mL
    25 mM 0.0784 mL 0.3918 mL 0.7836 mL 1.9589 mL
    30 mM 0.0653 mL 0.3265 mL 0.6530 mL 1.6324 mL
    40 mM 0.0490 mL 0.2449 mL 0.4897 mL 1.2243 mL
    50 mM 0.0392 mL 0.1959 mL 0.3918 mL 0.9795 mL
    60 mM 0.0326 mL 0.1632 mL 0.3265 mL 0.8162 mL
    80 mM 0.0245 mL 0.1224 mL 0.2449 mL 0.6122 mL
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    產(chǎn)品名稱：
    Defactinib
    目錄號(hào)：
    HY-12289
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