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  1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis
  3. Poziotinib

Poziotinib  (Synonyms: 波齊替尼; HM781-36B; NOV120101)

目錄號(hào): HY-15730 純度: 99.96%
COA 產(chǎn)品使用指南

HM781-36B 是一種口服活性,不可逆的泛 HER 抑制劑。HM781-36B 抑制 EGFRwt、HER-2 和 HER-4 的 IC50 值分別為 3.2、5.3 和 23.5 nM,對(duì)突變的 EGFR,包括 EGFRT790MEGFRL858R/T790M,IC50 值分別為 4.2 和 2.2 nM。具有良好的抗腫瘤活性。

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Poziotinib Chemical Structure

Poziotinib Chemical Structure

CAS No. : 1092364-38-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥860
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5 mg ¥800
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10 mg ¥1200
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50 mg ¥4200
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100 mg 現(xiàn)貨 詢價(jià)
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500 mg   詢價(jià)  

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Customer Review

    Poziotinib purchased from MCE. Usage Cited in: Cancers (Basel). 2020 Nov 4;12(11):3249.  [Abstract]

    Poziotinib, at 0.1, 0.3 and 0.6 μM, produces a significant decrease in the expression level of the ABCG2 transporter protein in S1-M1-80 cells after 72 h of incubation, compared to cells incubated with vehicle (0 μM). ABCG2 protein expression is significantly decreased in S1-M1-80 cells following incubation with 0.6 μM of Poziotinib for 48 or 72 h.
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity[1][2].

    IC50 & Target

    IC50: 3.2 nM (EGFRwt), 5.3 nM (HER-2), 23.5 nM (HER-4) 4.2 nM (EGFRT790M), 2.2 nM (EGFRL858R/T790M)[2]

    體外研究
    (In Vitro)

    The IC50 levels of Poziotinib (HM781-36B) for N87 and SNU216 were 0.001 and 0.004 μM, respectively, which was 10-1000 fold lower than the IC50 levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to ZD1839 or GW572016[1].
    Poziotinib (HM781-36B) also shows excellent selectivity with other kinases with greater than 100- to 1,000- fold IC50 values compared with EGFR family members. Poziotinib (HM781-36B) possesses a functional α,β‐unsaturated carbonyl group as Michael acceptor moiety at the C6 position that allows covalent modifications of the EGFR kinase domain active site[2].
    The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC50=0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX[3].

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

    體內(nèi)研究
    (In Vivo)

    The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only[1].

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

    分子量

    491.34

    Formula

    C23H21Cl2FN4O3

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    波齊替尼;波奇替尼;泊齊替尼

    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 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 50 mg/mL (101.76 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)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.0353 mL 10.1763 mL 20.3525 mL
    5 mM 0.4071 mL 2.0353 mL 4.0705 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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.87 mg/mL (5.84 mM); 澄清溶液

    • 方案 二

      請(qǐng)依序添加每種溶劑: 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.87 mg/mL (5.84 mM); 澄清溶液

    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

    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: 99.96%

    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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 2.0353 mL 10.1763 mL 20.3525 mL 50.8813 mL
    5 mM 0.4071 mL 2.0353 mL 4.0705 mL 10.1763 mL
    10 mM 0.2035 mL 1.0176 mL 2.0353 mL 5.0881 mL
    15 mM 0.1357 mL 0.6784 mL 1.3568 mL 3.3921 mL
    20 mM 0.1018 mL 0.5088 mL 1.0176 mL 2.5441 mL
    25 mM 0.0814 mL 0.4071 mL 0.8141 mL 2.0353 mL
    30 mM 0.0678 mL 0.3392 mL 0.6784 mL 1.6960 mL
    40 mM 0.0509 mL 0.2544 mL 0.5088 mL 1.2720 mL
    50 mM 0.0407 mL 0.2035 mL 0.4071 mL 1.0176 mL
    60 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8480 mL
    80 mM 0.0254 mL 0.1272 mL 0.2544 mL 0.6360 mL
    100 mM 0.0204 mL 0.1018 mL 0.2035 mL 0.5088 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:
    Poziotinib
    目錄號(hào):
    HY-15730
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