1. Immunology/Inflammation Apoptosis
  2. Interleukin Related Apoptosis
  3. SC144 hydrochloride

SC144 hydrochloride 

目录号: HY-15614A 纯度: 99.34%
COA 产品使用指南

SC144 hydrochloride 是首创的口服活性 gp130 (IL6-beta) 抑制剂。SC144 hydrochloride 结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进一步抑制下游靶基因的表达。SC144 hydrochloride 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 hydrochloride 诱导人卵巢癌细胞凋亡。

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SC144 hydrochloride Chemical Structure

SC144 hydrochloride Chemical Structure

CAS No. : 917497-70-2

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥990
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5 mg ¥900
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10 mg ¥1300
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25 mg ¥2400
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50 mg ¥4080
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100 mg ¥6950
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500 mg   询价  

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Other Forms of SC144 hydrochloride:

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Top Publications Citing Use of Products

    SC144 hydrochloride purchased from MCE. Usage Cited in: Inflamm Res. 2023 Jan 8.  [Abstract]

    SC144 (20 mg/kg; dissolved in DMSO; i.p.; single) significantly inhibits the expression of gp130 in mouse lung tissue.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells[1].

    IC50 & Target[1]

    IL6-beta

     

    体外研究
    (In Vitro)

    SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1].
    The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 μM) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer[1].
    SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells[1].
    SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner[1].
    SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis[1].

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

    Apoptosis Analysis[1]

    Cell Line: OVCAR-8 and Caov-3 cells
    Concentration: 2 μM
    Incubation Time: 24 hours
    Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells.

    Western Blot Analysis[1]

    Cell Line: OVCAR-8, Caov-3 cells
    Concentration: 0.5-2 μM
    Incubation Time: 0-6 hours
    Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.
    体内研究
    (In Vivo)

    SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts[1].
    SC144 (100 mg/kg; p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group[1].

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

    Animal Model: Athymic mice (human ovarian cancer xenograft)[1]
    Dosage: I.p; daily for 58 days
    Administration: 10 mg/kg
    Result: Significantly inhibited tumor growth by about 73%.
    分子量

    358.76

    Formula

    C16H12ClFN6O

    CAS 号
    性状

    固体

    颜色

    Light yellow to gray

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

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

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 10 mg/mL (27.87 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7874 mL 13.9369 mL 27.8738 mL
    5 mM 0.5575 mL 2.7874 mL 5.5748 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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    90% Corn Oil

      Solubility: ≥ 1 mg/mL (2.79 mM); 澄清溶液

      此方案可获得 ≥ 1 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 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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)。

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

    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: 99.34%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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 2.7874 mL 13.9369 mL 27.8738 mL 69.6845 mL
    5 mM 0.5575 mL 2.7874 mL 5.5748 mL 13.9369 mL
    10 mM 0.2787 mL 1.3937 mL 2.7874 mL 6.9684 mL
    15 mM 0.1858 mL 0.9291 mL 1.8583 mL 4.6456 mL
    20 mM 0.1394 mL 0.6968 mL 1.3937 mL 3.4842 mL
    25 mM 0.1115 mL 0.5575 mL 1.1150 mL 2.7874 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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    产品名称:
    SC144 hydrochloride
    目录号:
    HY-15614A
    需求量: