成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

  2. Protein Tyrosine Kinase/RTK
  3. FAK Pyk2
  4. PF-562271 besylate

PF-562271 besylate  (Synonyms: VS-6062 besylate)

目錄號: HY-10458 純度: 99.17%
COA 產(chǎn)品使用指南

PF-562271 (VS-6062) besylate 是有效，可逆，ATP競爭性的 FAK 和 Pyk2 激酶抑制劑，IC50 分別為 1.5 和 13 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

我們將采用定制合成服務(wù)的方式為您快速提供所需產(chǎn)品和技術(shù)服務(wù)

PF-562271 besylate Chemical Structure

PF-562271 besylate Chemical Structure

CAS No. : 939791-38-5

1.  客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1092
In-stock
1 mg ￥321
In-stock
5 mg ￥746
In-stock
10 mg ￥1288
In-stock
25 mg ￥2213
In-stock
50 mg ￥3238
In-stock
100 mg ￥4625
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Other Forms of PF-562271 besylate:

    PF-562271 besylate purchased from MCE. Usage Cited in: Cell Death Dis. 2023 Feb 24;14(2):157.  [Abstract]

    PF-562271 (250 nM; 6 h) largely inhibits Akt-S6 phosphorylation in OE-MXRA5 priPC-1 cells.

    PF-562271 besylate purchased from MCE. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59.  [Abstract]

    786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.

    PF-562271 besylate purchased from MCE. Usage Cited in: Practical Oncology Journal. 2015, 29(5): 444-449.

    Effects and mechanism of Biglycan and FAK signaling pathway on the invasion and metastasis of colon cancer cells.

    PF-562271 besylate purchased from MCE. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83.  [Abstract]

    FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.

    • 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

    PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively[1].

    IC50 & Target

    IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 GI50
    2.1 μM
    Compound: PF-562271
    Antiproliferative activity against human A549 cells after 2 days by spectrophotometric analysis
    Antiproliferative activity against human A549 cells after 2 days by spectrophotometric analysis
    		[PMID: 30340900]
    HeLa GI50
    1.7 μM
    Compound: PF-562271
    Antiproliferative activity against human HeLa cells after 2 days by spectrophotometric analysis
    Antiproliferative activity against human HeLa cells after 2 days by spectrophotometric analysis
    		[PMID: 30340900]
    HepG2 GI50
    1.2 μM
    Compound: PF-562271
    Antiproliferative activity against human HepG2 cells after 2 days by spectrophotometric analysis
    Antiproliferative activity against human HepG2 cells after 2 days by spectrophotometric analysis
    		[PMID: 30340900]
    OVCAR-3 GI50
    1.8 μM
    Compound: PF-562271
    Antiproliferative activity against human OVCAR3 cells after 2 days by spectrophotometric analysis
    Antiproliferative activity against human OVCAR3 cells after 2 days by spectrophotometric analysis
    		[PMID: 30340900]
    U-87MG ATCC GI50
    3.7 μM
    Compound: PF-562271
    Antiproliferative activity against human U87MG cells after 2 days by spectrophotometric analysis
    Antiproliferative activity against human U87MG cells after 2 days by spectrophotometric analysis
    		[PMID: 30340900]
    體外研究
    (In Vitro)

    PF-562271 (VS-6062) besylate 是重組酶測定中 cdk2/E、cdk5/p35、cdk1/B 和 cdk3/E 的 30 至 120 nM (15.2 至 60.1 ng/mL) 抑制劑[1]。PF-562，271 阻斷 bFGF 刺激的血管生成，如在雞絨毛尿囊膜測定中所進(jìn)行的[2]。觀察到用 PF-562271 處理細(xì)胞或通過 siRNA 敲低 FAK 可增加細(xì)胞間粘附強(qiáng)度[3]。

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

    PF-562271 (33 mg/kg，po) 在荷瘤小鼠中以劑量和時(shí)間依賴性方式抑制腫瘤中的 FAK 磷酸化。相對于 PF-562271 總血濃度的 FAK 磷酸化抑制導(dǎo)致計(jì)算出的 EC50 為 93 ng/mL。在第 3 天，PF-562271 (25 mg/kg，口服) 在處理的腫瘤中誘導(dǎo)的細(xì)胞凋亡比載體處理的對照腫瘤高 2 倍[1]。PF-562271 (33 mg/kg，口服) 和達(dá)沙替尼廣泛抑制動(dòng)物體內(nèi)腫瘤細(xì)胞的移動(dòng)。用 PF-562271 處理后抑制 FAK 激酶活性會(huì)導(dǎo)致體內(nèi) E-鈣粘蛋白動(dòng)力學(xué)改變[3]。

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

    665.66

    Formula

    C27H26F3N7O6S2
    CAS 號
    性狀

    固體

    顏色

    Off-white to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 21.4 mg/mL (32.15 mM; 超聲加熱助溶; 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)

    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 1.5023 mL 7.5113 mL 15.0227 mL
    5 mM 0.3005 mL 1.5023 mL 3.0045 mL
    查看完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?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

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

      Solubility: ≥ 1.67 mg/mL (2.51 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲(chǔ)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: ≥ 1.67 mg/mL (2.51 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲(chǔ)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(dòng)物溶解方案計(jì)算器
    請輸入動(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）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)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(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，請謹(jǐn)慎選擇該方案。
    請確保第一步儲(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: 99.17%

    參考文獻(xiàn)
    Kinase Assay
    [1]

    Briefly, purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2] for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2mol/LH2SO4). IC50 values are determined using the Hill-Slope Model.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×106 cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of appr 150 mm3?in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm3) is measured with Vernier calipers and calculated. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used.

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

    PF-562271 besylate 相關(guān)分類

    完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?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 1.5023 mL 7.5113 mL 15.0227 mL 37.5567 mL
    5 mM 0.3005 mL 1.5023 mL 3.0045 mL 7.5113 mL
    10 mM 0.1502 mL 0.7511 mL 1.5023 mL 3.7557 mL
    15 mM 0.1002 mL 0.5008 mL 1.0015 mL 2.5038 mL
    20 mM 0.0751 mL 0.3756 mL 0.7511 mL 1.8778 mL
    25 mM 0.0601 mL 0.3005 mL 0.6009 mL 1.5023 mL
    30 mM 0.0501 mL 0.2504 mL 0.5008 mL 1.2519 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.

    您最近查看的產(chǎn)品:

    Your information is safe with us. * Required Fields.

       產(chǎn)品名稱：

    		  

    * 需求量：

    * 客戶姓名：

    		 

    * Email：

    * 電話：

    		 

    * 公司或機(jī)構(gòu)名稱：

       留言給我們：

    Bulk Inquiry

    Inquiry Information

    產(chǎn)品名稱：
    PF-562271 besylate
    目錄號：
    HY-10458
    需求量：