1. MAPK/ERK Pathway
  2. JNK
  3. Bentamapimod

Bentamapimod  (Synonyms: AS 602801)

目录号: HY-14761 纯度: 99.32%
COA 产品使用指南

Bentamapimod (AS 602801) 是一种ATP竞争性的 JNK 抑制剂,作用于 JNK1JNK2JNK3IC50 分别为 80 nM,90 nM 和 230 nM。

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Bentamapimod Chemical Structure

Bentamapimod Chemical Structure

CAS No. : 848344-36-5

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10 mM * 1 mL in DMSO ¥770
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5 mg ¥700
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10 mg ¥1200
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50 mg ¥2500
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Top Publications Citing Use of Products

    Bentamapimod purchased from MCE. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617.   [Abstract]

    A2780 CSLCs are treated with paclitaxel (2 nM) or carboplatin (5 μM) in the presence or absence of AS602801 (7.5 μM) and/or YM155 (10 nM) for 3 days, and then subjected to western blot analysis of survivin and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

    Bentamapimod purchased from MCE. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617.   [Abstract]

    A2780 CSLCs and TOV-21G CLSCs are treated with AS602801 at 7.5 μM for the indicated time and the cells are subjected to western blot analysis of multidrug resistance protein 1 (MDR1) and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

    Bentamapimod purchased from MCE. Usage Cited in: Anticancer Res. 2018 Dec;38(12):6699-6706.  [Abstract]

    The protein expression of analysis Survivin with or without the treatment of AS602801 in different times and concentrations.

    Bentamapimod purchased from MCE. Usage Cited in: Oncotarget. 2016 May 10;7(19):27021-32.  [Abstract]

    AS602801 treatment causes loss of stem cell marker expression in cancer stem cells. Subsequent analysis revealed that the levels of other stem cell markers, such as Sox2, Nanog, and Bmi1, are decreased similarly to CD133.

    查看 JNK 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

    Bentamapimod (AS 602801) is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.

    IC50 & Target[1]

    JNK1

    80 nM (IC50)

    JNK2

    90 nM (IC50)

    JNK3

    230 nM (IC50)

    体外研究
    (In Vitro)

    Bentamapimod (AS 602801) 处理诱导细胞死亡,并相应地以剂量依赖性方式减少所有三种细胞系中的活细胞数量,表明 Bentamapimod (AS 602801) 可能对肿瘤细胞具有选择性细胞毒活性。Bentamapimod (AS 602801) 在不降低正常人成纤维细胞活力的浓度下,对血清培养的非干细胞癌细胞和源自人胰腺癌、非小细胞肺癌、卵巢癌和胶质母细胞瘤的癌症干细胞均表现出细胞毒性. Bentamapimod (AS 602801) 还抑制在 Bentamapimod (AS 602801) 处理后存活的癌症干细胞的自我更新和肿瘤启动能力[2]

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

    体内研究
    (In Vivo)

    用 30 mg/kg Bentamapimod (AS 602801) 处理携带从患有子宫内膜异位症 (BWE) 的女性进行活检的异种移植物的裸鼠导致 29% 的病变消退。单独使用醋酸甲羟孕酮 (MPA) 或孕酮 (PR) 不会导致 BWE 病变消退,但将 10 mg/kg Bentamapimod (AS 602801) 与 MPA 联合使用可导致 38% 的病变消退。在人类子宫内膜器官培养物 (来自健康女性) 中,用 Bentamapimod (AS 602801) 或 MPA 处理可减少基质金属蛋白酶 3 (MMP-3) 释放到培养基中。在用 BWE 建立的器官培养物中,PR 或 MPA 未能抑制 MMP-3 分泌,而单独的 AS 602801 或 MPA + Bentamapimod (AS 602801) 抑制 MMP-3 的产生。在自体大鼠子宫内膜异位症模型中,与 GnRH 拮抗剂 Antide (84%) 相比,AS 602801 可使病变消退 48%。Bentamapimod (AS 602801) 减少子宫内膜异位病变中的炎性细胞因子,而同侧角中的细胞因子水平不受影响。此外,Bentamapimod (AS 602801) 可增强自然杀伤细胞活性,而对子宫没有明显的负面影响[3]

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

    分子量

    457.55

    Formula

    C25H23N5O2S

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 8.33 mg/mL (18.21 mM; 超声助溶 (<60°C); 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 2.1856 mL 10.9278 mL 21.8555 mL
    5 mM 0.4371 mL 2.1856 mL 4.3711 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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: ≥ 0.83 mg/mL (1.81 mM); 悬浊液

      此方案可获得 ≥ 0.83 mg/mL(饱和度未知)的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 8.3 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。
    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: 99.32%

    参考文献
    Cell Assay
    [2]

    PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of Bentamapimod (AS 602801) (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye[2].

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

    Animal Administration
    [3]

    Mice[3]
    The 5-week-old athymic (ncr/nude) ovariectomized mice are anesthetized with isoflurane and subcutaneously implanted with a silastic capsule containing 8 μg estradiol. Twenty-four hours later, mice received subcutaneous or intraperitoneal injection with a phosphate-buffered saline (PBS) suspension of 8 to 10 human endometrial tissue fragments/mouse (biopsies obtained from volunteers or patients) on the ventral midline just below the umbilicus. For 24 hours immediately preceding injection, tissue fragments are established as organ cultures treated with 1 nM estradiol, PR, or MPA. Oral administration of Bentamapimod (AS 602801) is initiated 10 to 12 days following the injection of tissue. Progesterone is provided via a slow-release silastic capsule containing 25 μg PR, and MPA is given by twice-weekly injections (200 mg/kg) along the right flank using a tuberculin syringe. Bentamapimod (AS 602801) is administered by gavage at a dose of 10 mg/kg and 30 mg/kg/animal for 30 days. Following the completion of treatment, mice are again anesthetized and sacrificed by cervical dislocation for direct examination of lesion size and number. Uteri are measured and weighed, and excised lesions rapidly frozen for further analysis[3].

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

    参考文献

    Bentamapimod 相关分类

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1856 mL 10.9278 mL 21.8555 mL 54.6388 mL
    5 mM 0.4371 mL 2.1856 mL 4.3711 mL 10.9278 mL
    10 mM 0.2186 mL 1.0928 mL 2.1856 mL 5.4639 mL
    15 mM 0.1457 mL 0.7285 mL 1.4570 mL 3.6426 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.

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    目录号:
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