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  2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. Antifolate Autophagy Apoptosis
  4. Pemetrexed disodium

Pemetrexed disodium  (Synonyms: 培美曲塞二鈉鹽; LY231514 disodium)

目錄號(hào): HY-10820A 純度: 99.95%
COA 產(chǎn)品使用指南 技術(shù)支持

Pemetrexed disodium (LY231514 disodium) 是一種葉酸拮抗劑 (antifolate)。Pemetrexed disodium 抑制胸苷酸合成酶 (TS)，二氫葉酸還原酶 (DHFR) 和甘氨酰胺核苷酸甲酰轉(zhuǎn)移酶 (GARFT) 的 Ki 分別為 1.3 nM，7.2 nM 和 65 nM。

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Pemetrexed disodium Chemical Structure

Pemetrexed disodium Chemical Structure

CAS No. : 150399-23-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in Water ￥605
In-stock
1 mg ￥171
In-stock
5 mg ￥343
In-stock
10 mg ￥550
In-stock
50 mg ￥750
In-stock
100 mg ￥1250
In-stock
200 mg ￥2100
In-stock
500 mg   詢(xún)價(jià)  
1 g   詢(xún)價(jià)  

* Please select Quantity before adding items.

Other Forms of Pemetrexed disodium:

    Pemetrexed disodium purchased from MCE. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060.  [Abstract]

    Immunofluorescence assay showing the expression and intracellular location of UCHL1 in NSCLC cells. Increased UCHL1 levels are observed in both the cytoplasm and the nucleus of the PEM-R cells.

    Pemetrexed disodium purchased from MCE. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060.  [Abstract]

    Western blot analysis of UCHL1 levels in PEM-R cells and their parental cells. The mRNA and protein levels of UCHL1 in the PEM-R cells are significantly increased, relative to in the parental 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

    Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].

    IC50 & Target

    Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    3.29 μM
    Compound: 3; PTX
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30927565]
    GES1 CC50
    22.62 μM
    Compound: 3; PTX
    Cytotoxicity against human GES-1 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human GES-1 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30927565]
    HepG2 IC50
    3.73 μM
    Compound: 3; PTX
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30927565]
    L02 CC50
    30.69 μM
    Compound: 3; PTX
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30927565]
    OVCAR-3 IC50
    4.35 μM
    Compound: 3; PTX
    Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Antiproliferative activity against human OVCAR3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30927565]
    SGC-7901 IC50
    6.96 μM
    Compound: 3; PTX
    Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30927565]
    體外研究
    (In Vitro)

    Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (Km=1.6 μM and Vmax/Km=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (Ki=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (Ki=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors[1].

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

    The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment[2].

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

    471.37

    Formula

    C20H19N5Na2O6
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱(chēng)

    培美曲塞二鈉鹽
    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)： 

    H2O 中的溶解度 : 100 mg/mL (212.15 mM; 超聲助溶 (<60°C))

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.1215 mL 10.6074 mL 21.2148 mL
    5 mM 0.4243 mL 2.1215 mL 4.2430 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 (sealed storage, away from moisture)。-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。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 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)：

    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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： PBS

      Solubility: 50 mg/mL (106.07 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： Saline

      Solubility: 100 mg/mL (212.15 mM); 澄清溶液; 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(guò)程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.95%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC50). Pemetrexed is dissolved initially in DMSO at a concentration of 4 mg/mL and further diluted with cell culture medium to the desired concentration. CCRF-CEM leukemia cells in complete medium are added to 24-well Cluster plates at a final concentration of 4.8×104 cells/well in a total volume of 2 mL. Test compounds at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 h at 37°C in an atmosphere of 5% CO2 in air. At the end of the incubation, cell numbers are determined on a ZBI Coulter counter. Control wells usually contain 4×105 to 6×105 cells at the end of the incubation. For several studies, IC50s are determined for each compound in the presence of either 300 μM AICA, 5 μM thymidine, 100 μM hypoxanthine, or combination of 5 μM hymidine plus 100 μM hypoxanthine[1].

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

    Mice[2]
    Female CBA mice and female NOD/SCID mice (NOD.CB17-Prkdcscid) at 6-8 wk of age are used. Premetrexed (100 mg/kg) is given i.p. from days 4-8 (5 consecutive d) to tumor-bearing mice to explore the synergistic effect when combined with anti-CD25 Ab or IgG control. The dose and schedule used for Pemetrexed in the current study is determined based on previous studies in mice.

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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
    H2O 1 mM 2.1215 mL 10.6074 mL 21.2148 mL 53.0369 mL
    5 mM 0.4243 mL 2.1215 mL 4.2430 mL 10.6074 mL
    10 mM 0.2121 mL 1.0607 mL 2.1215 mL 5.3037 mL
    15 mM 0.1414 mL 0.7072 mL 1.4143 mL 3.5358 mL
    20 mM 0.1061 mL 0.5304 mL 1.0607 mL 2.6518 mL
    25 mM 0.0849 mL 0.4243 mL 0.8486 mL 2.1215 mL
    30 mM 0.0707 mL 0.3536 mL 0.7072 mL 1.7679 mL
    40 mM 0.0530 mL 0.2652 mL 0.5304 mL 1.3259 mL
    50 mM 0.0424 mL 0.2121 mL 0.4243 mL 1.0607 mL
    60 mM 0.0354 mL 0.1768 mL 0.3536 mL 0.8839 mL
    80 mM 0.0265 mL 0.1326 mL 0.2652 mL 0.6630 mL
    100 mM 0.0212 mL 0.1061 mL 0.2121 mL 0.5304 mL

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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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(chēng)：
    Pemetrexed disodium
    目錄號(hào)：
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