1. PROTAC Apoptosis
  2. Ligands for E3 Ligase Molecular Glues Apoptosis
  3. Pomalidomide

Pomalidomide  (Synonyms: 泊马度胺; CC-4047)

目录号: HY-10984 纯度: 99.85%
COA 产品使用指南

Pomalidomide 是第三代免疫调节剂,以分子胶的方式作用。Pomalidomide 与 E3 连接酶 cereblon 相互作用,诱导必需的 Ikaros 转录因子的降解。

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Pomalidomide Chemical Structure

Pomalidomide Chemical Structure

CAS No. : 19171-19-8

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10 mM * 1 mL in DMSO ¥616
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Top Publications Citing Use of Products

    Pomalidomide purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Pomalidomide purchased from MCE. Usage Cited in: Gen Comp Endocrinol. 2015 Dec 30;228:1-8.  [Abstract]

    TNFα significantly inhibits the mRNA and protein expression of GSK-3β, while POM significantly induces the mRNA and protein expression of GSK-3β (A). The mRNA and protein expression of β-catenin is significantly induced by TNFα, but significantly inhibited by POM (B). The protein expression of PPARγ and C/EBPα is significantly inhibited by TNFα, while significantly induced by POM treatment (C and D).

    查看 Ligands for E3 Ligase 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

    IC50 & Target[5]

    Cereblon

     

    体外研究
    (In Vitro)

    Pomalidomide 还抑制全血 TNF-α,IC50 为 25 nM[1]。与载体处理的对照相比,将淋巴瘤细胞暴露于 Pomalidomide (CC-4047) 会导致细胞增殖减少 40%。Pomalidomide 抑制 Raji 细胞 40% 的 DNA 合成 (P=0.036)[2]。在 CD4+ 和 CD8+ 细胞中,Pomalidomide (CC-4047) 是最有效的 IL-2 升高剂,其次是 CC-6032 和 CC-5013。Pomalidomide 在升高 IL-2、IL-5 和 IL-10 方面明显强于 CC-5013,在升高 IFN-γ 方面略强于 CC-5013[3]

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

    体内研究
    (In Vivo)

    在 mAb 处理前连续两天给予 Pomalidomide (CC-4047) 可增强利妥昔单抗的抗肿瘤活性,并使荷淋巴瘤小鼠的中位生存期增加一倍。在统计学上,观察到用 Rituximab 处理的动物与 Pomalidomide + Rituximab 处理的动物之间存在显著差异。接受 Pomalidomide 和利妥昔单抗处理的动物的中位生存时间 (中位生存期,74 天;95% CI,70-78) 长于接受利妥昔单抗单一疗法处理的动物 (中位生存期,38 天;95% CI,26-50;log-秩检验,P=0.002)。如流式细胞术分析所示,在荷淋巴瘤 SCID 小鼠中,连续两天施用 CC-5013 或 Pomalidomide 会导致循环 NK 细胞数量显著增加[2]。对大鼠口服 Pomalidomide (POM) 50 mg/kg 后,血液中未结合的浓度在 4.6±2.4 小时时达到 1100±82 ng/mL 的 Cmax 值,同时 AUC(0-10) 值为 6800 ng?hr/mL。然而,大脑中未结合的 POM 在 4.1h 时的 Cmax 值为 430 ng/mL,AUC(0-10) 值为 2700 ng?hr/mL,未结合的 AUCbrain 与 AUCblood 的比率为 0.39。这些值与出色的血脑屏障穿透力一致。本研究中获得的结果与同时进行的研究中观察到的结果一致,该研究观察了小鼠口服 POM 后的全脑内容[4]

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

    Clinical Trial
    分子量

    273.24

    Formula

    C13H11N3O4

    CAS 号
    性状

    固体

    颜色

    Light yellow to green yellow

    中文名称

    泊马度胺

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (182.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.6598 mL 18.2989 mL 36.5979 mL
    5 mM 0.7320 mL 3.6598 mL 7.3196 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (9.15 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (9.15 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: 0.5% CMC-Na  0.5% Tween-80

      Solubility: 10 mg/mL (36.60 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.96%

    参考文献
    Cell Assay
    [2]

    Lymphoma cell lines are placed in 96-well plates (1×105 cells per well) and exposed to escalating concentrations of CC-5013, Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL), or vehicle control single agents or in combination with Rituximab or Trastuzumab (isotype), at a final antibody concentration of 10 μg/mL. The final concentration is adjusted to 200 μL with 10% RPMI. The cell lines are incubated at 37°C and 5% CO2 for 24 and 48 hours. Following 24 or 48 hours, 1 μCi per well of [3H]-thymidine is added and cells are incubated for 18 hours more. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter. Each experiment is done in triplicate at three different times; results are presented as the mean of counts per minute (cpm) at 24 and 48 hours±SD[2].

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

    Animal Administration
    [2][4]

    Mice[2]
    Six- to 8-week-old SCID mice are used for this purpose. On day 0, all the animals receive 1×106 Raji cells via tail vein injection. After 72 hours of tumor engraftment, the animals are divided into seven cohorts. The first cohort (group A) serve as control and receive no treatment. Groups B and C consist of animals treated with either CC-5013 (0.5 mg/kg) or Pomalidomide (0.5 mg/kg) given i.p. on days +3, +4, +8, +9, +13, +14, +18, and +19. Groups D and E are treated with Rituximab or Trastuzumab (isotype control) monotherapy given via tail vein injection at 10 mg/kg on days +5, +10, +15, and +20. Finally, groups F and G consist of animals treated with Rituximab in combination with CC-5013 (group E) or Pomalidomide (group G). IMiDs are given i.p. for two consecutive days before each dose of Rituximab. After completion of therapy, animals are observed for a period of 90 days. The end point of the study is survival defined as the time for the development of limb paralysis. Animals that reach the end point or survived after 3 months of observation are sacrificed by cervical dislocation. Pathologic examination of all organs (liver, lung, and brain) is done to detect any residual disease. The experiments are repeated in three separate occasions.
    Rats[4]
    A total of 3 male CD-IGS rats are used. Pomalidomide is administered as a single PO administration via the stomach cannula, at 50 mg/kg (5 mL/kg) in a 0.5% carboxymethylcellulose/0.25% Tween 80 suspension formulation. Microdialysate is collected in a cooling fraction collector, set at 4°C at intervals of 25 minutes for 10 hours after dosing. To calculate AUC, the corrected concentration of each sample is multiplied by the interval over which the sample is collected; in this case 25 minutes, and divided by 60 minutes per hour. The sum of these values represented the total AUC value over the specified time range. To generate graphs, the concentration at each time point is plotted at the mid-point of each collection interval. Microdialysates are collected at the specified time points and analyzed for Pomalidomide concentration using a LC-MS/MS assay, within 12 hours.

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

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.6598 mL 18.2989 mL 36.5979 mL 91.4947 mL
    5 mM 0.7320 mL 3.6598 mL 7.3196 mL 18.2989 mL
    10 mM 0.3660 mL 1.8299 mL 3.6598 mL 9.1495 mL
    15 mM 0.2440 mL 1.2199 mL 2.4399 mL 6.0996 mL
    20 mM 0.1830 mL 0.9149 mL 1.8299 mL 4.5747 mL
    25 mM 0.1464 mL 0.7320 mL 1.4639 mL 3.6598 mL
    30 mM 0.1220 mL 0.6100 mL 1.2199 mL 3.0498 mL
    40 mM 0.0915 mL 0.4575 mL 0.9149 mL 2.2874 mL
    50 mM 0.0732 mL 0.3660 mL 0.7320 mL 1.8299 mL
    60 mM 0.0610 mL 0.3050 mL 0.6100 mL 1.5249 mL
    80 mM 0.0457 mL 0.2287 mL 0.4575 mL 1.1437 mL
    100 mM 0.0366 mL 0.1830 mL 0.3660 mL 0.9149 mL
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    目录号:
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