1. TGF-beta/Smad Autophagy
  2. TGF-β Receptor Autophagy
  3. LY2109761

LY2109761是可口服,选择性的 TGF-β receptor type I/II 抑制剂,Ki分别为38 nM 和 300 nM。

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LY2109761 Chemical Structure

LY2109761 Chemical Structure

CAS No. : 700874-71-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880
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1 mg ¥314
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5 mg ¥800
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10 mg ¥1400
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50 mg ¥4300
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100 mg ¥6500
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200 mg ¥9238
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500 mg   询价  
1 g   询价  

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 43 篇科研文献

WB

    LY2109761 purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836.  [Abstract]

    LY2109761 at 100 nM, 10 μM, or 50 μM is added for 30 min to block TGFβR1/2 prior to TGF-β1-treatment, then proteins are collected, and the levels of Sphk2, fibronectin, and α-SMA are detected by Western blotting.

    LY2109761 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov;103:173-181.  [Abstract]

    TRPM7 mRNA and protein expressions are effectively suppressed by LY2109761 and SIS3 in ASMCs compared with those in 10 ng/mL TGF-β1-stimulated cells.

    LY2109761 purchased from MCE. Usage Cited in: Cell Biol Int. 2017 Sep;41(9):960-968.  [Abstract]

    The phosphorylation level of Smad2 is significantly inhibited by LY2109761. The M2 macrophage-induced increase of α-SMA and decrease of E-cadherin and CK-18 are inhibited by LY2109761.

    LY2109761 purchased from MCE. Usage Cited in: J Hepatol. 2015 Oct;63(4):863-73.  [Abstract]

    Blocking the TGF-beta and ERK signalling effectively inhibits EDIL3 mediated angiogenesis and invasion. Western blotting analysis of the expression of p-ERK and p-Smad2 in DMSO- and VX-11e or LY2109761-treated HuH7-p-lenti-EDIL3 cells. GAPDH is used as a loading control.

    LY2109761 purchased from MCE. Usage Cited in: Int J Mol Med. 2015 Jun;35(6):1667-74.  [Abstract]

    Inhibition of the TGF-β1/Smad2 pathway decreases H2O2-induced human umbilical vein endothelial cell (HUVEC) apoptosis, but not oxidative stress. Western blot analysis is performed to determine protein expression in the HUVECs in the control, model, AST Ⅳ and LY2109761 groups.

    查看 TGF-β Receptor 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

    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.

    IC50 & Target

    Ki: 38 nM (TβRI), 300 nM (TβRII)

    体外研究
    (In Vitro)

    LY2109761 以剂量依赖性方式显著抑制 L3.6pl/GLT 软琼脂菌落的生长,在 2 μM 时抑制约 33%,在 20 μM 时抑制约 73%。用 LY2109761 (5 μM) 靶向 TβRI/II 激酶活性几乎完全抑制 L3.6pl/GLT 细胞的基础迁移和 TGF-β1 刺激的迁移[1]
    LY2109761 诱导 Smad-2 磷酸化的剂量依赖性降低。LY2109761 抑制 Smad-2 的 HLE 内源性磷酸化。LY2109761 通过 3 维结构阻断不同 ECM 蛋白的迁移以及 HLE 和 HLF 的侵入。LY2109761 在 24 小时后增加 E-钙粘蛋白 mRNA 表达,在 48 小时后增加蛋白质水平[2]
    LY2109761 预处理降低了辐射后 U87MG 和 T98 细胞培养物中的克隆形成存活率,导致放射敏感性增加,DEF0.1 分别为 1.30 和 1.37[3]

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

    体内研究
    (In Vivo)

    LY2109761 (50 mg/kg,po) 大大减小肿瘤体积并将小鼠的中位生存期延长至 45.0 天。用 LY2109761 处理的小鼠发生的转移性病灶明显减少,并且在其中一些小鼠中,如 GFP 信号所示,在腹部未发现转移性病灶[1]
    LY2109761 在 BALB/c 裸鼠 U87MG 皮下异种移植肿瘤模型中增强辐射诱导的肿瘤生长延迟。LY2109761 提高原位 CSLC 胶质母细胞瘤模型的存活率并增强辐射的抗肿瘤活性[2]

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

    分子量

    441.52

    Formula

    C26H27N5O2

    CAS 号
    性状

    固体

    颜色

    White 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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 6.67 mg/mL (15.11 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 2.2649 mL 11.3245 mL 22.6490 mL
    5 mM 0.4530 mL 2.2649 mL 4.5298 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: ≥ 2.08 mg/mL (4.71 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.71 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    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 (22.65 mM); Suspened solution; 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: 99.91%

    参考文献
    Cell Assay
    [1]

    L3.6pl/GLT cells are washed twice with cold PBS and lysed at 4°C into RIPA buffer (50 mM Tris HCl [pH 8], 150 mM NaCl, 1% NP-40, 0.5% sodium deoxycolate, and 0.1% SDS). Tumor and liver specimens are homogenized into RIPA buffer with an electric homogenizer and then maintained in constant agitation for two hours at 4°C. The lysates are cleared by centrifugation. Each lysate (20 µg of protein) is separated by 8% SDS-PAGE and probed with polyclonal rabbit antibodies against total ERK1/2, TβRI, and TβRII or with monoclonal mouse antibodies against phosphorylated Smad2, total Smad2, phosphorylated ERK1/2, and phosphorylated and total JNK. Immunoreactive proteins are visualized with Lumi-Light Western blotting substrate according to the manufacturer's instructions. phosphorylated Smad2/Smad2 band density ratios are calculated using the ImageQuant software.

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

    Animal Administration
    [1]

    Fifty mice are randomLy allocated into five groups (n=5 mice per group) to receive p.o. vehicle for 50 μL of LY2109761 or 50 mg/kg LY2109761 twice a day p.o. On day 0, mice are anesthetized with 1.5% isofluorane-air mixture, a small left abdominal flank incision is created, and the spleen is carefully exteriorized. L3.6pl/GLT or C5LM2/GLT cells (1.0×105 cells/50 μL of HBSS), cultured in the presence of LY2109761 (5 μM) or DMSO from day −5 to day 0, are inoculated into the spleen with a 30-gauge needle. A visible paling of the spleen is the criterion for successful inoculation. After 10 min, the spleen is removed using a high-temperature cautery to avoid the possibility that the ectopic growth of pancreatic tumor cells in the spleen could be a confounding source of hematogenous liver metastatic cells. The abdominal wall is closed in one layer with wound clips. Treatment with 50 mg/kg LY2109761 twice a day p.o. (days 1-5 of each week after inoculation) is continued for one group of untreated mice inoculated with untreated cells.

    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 2.2649 mL 11.3245 mL 22.6490 mL 56.6226 mL
    5 mM 0.4530 mL 2.2649 mL 4.5298 mL 11.3245 mL
    10 mM 0.2265 mL 1.1325 mL 2.2649 mL 5.6623 mL
    15 mM 0.1510 mL 0.7550 mL 1.5099 mL 3.7748 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:
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    目录号:
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