1. JAK/STAT Signaling Autophagy Apoptosis
  2. Pim Autophagy Apoptosis
  3. SGI-1776 free base

SGI-1776 free base 

目录号: HY-13287 纯度: 99.23%
COA 产品使用指南

SGI-1776 free base 是一种 Pim 抑制剂,抑制 Pim-1,Pim-2 和 Pim-3 的活性,IC50 值分别为 7 nM,363 nM 和 69 nM。

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SGI-1776 free base Chemical Structure

SGI-1776 free base Chemical Structure

CAS No. : 1025065-69-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1135
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1 mg ¥469
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5 mg ¥1032
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10 mg ¥1989
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50 mg ¥4938
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Other Forms of SGI-1776 free base:

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Top Publications Citing Use of Products

    SGI-1776 free base purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 22;9(3):307.  [Abstract]

    PIM1 directly phosphorylated Smad2 and Smad3 and that inhibition of PIM1 kinase activity with SGI-1776 significantly reduces the protein levels of p-Smad2 and p-Smad3
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.

    IC50 & Target

    Ki: 7 nM (Pim-1), 363 nM (Pim-2), 69 nM (Pim-3)[4]

    体外研究
    (In Vitro)

    SGI-1776 free base (2.5, 5 μM) 抑制 SACC 细胞中的 Pim-1 蛋白表达和 Pim-1 激酶活性。SGI-1776 free base (2.5, 5 μM) 在 SACC-83 和 SACC-LM 细胞中引起细胞周期停滞并减少细胞增殖[1]
    SGI-1776 free base (5 μM) 抑制 SACC-83 和 SACC-LM 细胞的细胞迁移和侵袭[1]
    SGI-1776 free base (0、2.5 或 5 μM) 通过激活 Caspase-3 诱导细胞凋亡[1]
    SGI-1776 free base (5 µM) 在不影响脂肪细胞数量的情况下对脂质积累和 TG 合成均有抑制作用[2]
    SGI-1776 free base (5 µM) 抑制脂肪形成,特别是在分化的早期阶段。 SGI-1776 free base (5 µM) 在脂肪细胞分化过程中降低 C/EBP-α 和 PPAR-γ 的表达以及 STAT-3 的磷酸化水平,并在脂肪细胞分化过程中下调 FAS、瘦素和 RANTES 的蛋白质和/或 mRNA 表达 脂肪细胞分化[2]
    SGI-1776 free base 对 HO-8910 细胞表现出显着的剂量依赖性活性,IC50为 (5.2±0.6) µM,SGI-1776 free base 的抑制作用为 在体外从 1.25 µM 急剧增加到 20 µM[3]
    SGI-1776 free base 以剂量依赖的方式抑制 HO-8910 细胞的迁移和侵袭,5 μM 时抑制迁移和侵袭的率为[3]
    SGI-1776 free base (2.5、5 和 10 µM) 以剂量依赖的方式降低 HO-8910 细胞的 Pim-1 激酶活性。 此外,SGI-1776 free base 下调 Pim-1 表达显着抑制细胞活力,使细胞停滞在 G1 期,抑制迁移和侵袭[3]

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

    体内研究
    (In Vivo)

    SGI-1776 free base (75, 200 mg/kg, 口服) 在小鼠的 MV-4-11 异种移植模型中,以剂量依赖性方式表现出有效且持续的抗肿瘤活性[4]

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

    Clinical Trial
    分子量

    405.42

    Formula

    C20H22F3N5O

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

    DMSO 中的溶解度 : 125 mg/mL (308.32 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 2.4666 mL 12.3329 mL 24.6658 mL
    5 mM 0.4933 mL 2.4666 mL 4.9332 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: ≥ 2.08 mg/mL (5.13 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 (5.13 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。
    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: 99.23%

    参考文献
    Kinase Assay
    [1]

    SACC-83 free base and SACC-LM cells of 0 μM, 2.5 μM and 5 μM groups after SGI-1776 exposure are harvested. 6 samples of SACC cells are diluted in Kinase buffer and pipetted into the wells which is pre-coated with a substrate corresponding to recombinant p21waf1. It contains threonine residues that can be efficiently phosphorylated by Pim-1. After undergoing the procedure, measure absorbance in each well is quantitated by spectrophotometry at dual wavelengths of 450/540 nm. It reflects the relative amount of Pim-1 activity in the 6 groups of SACC cells.

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

    Cell Assay
    [3]

    Cells are seeded in a 96-well plate at a density of 5 000 cells/well. After incubation for 24 h, different concentrations of SGI-1776 (0.625, 1.25, 2.5, 5, 10, 20, 40 µM) are added to each well and cultured for 48 h. The medium is removed and then incubated with 5 mg/L MTT for 4 h. Next, the supernatant is removed after centrifugation. Finally, 100 µL of DMSO is added and an absorbance at 570 nm wavelength (A570) is measured by enzyme-labeling instrument. Relative cell proliferation inhibition rate (IR)=(1-average A570 of the experimental group/average A570 of the control group)×100%.

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

    Animal Administration
    [4]

    The conditions for animal room environment and photoperiod are 20-25°C, 40%-70% humidity, and 12 hours of light/12 hours of dark cycle. Each mouse is inoculated subcutaneously at the right flank with MV-4-11 tumor cells (5×106). The treatments start when the tumor size reach 80-150 mm3. Mice are randomized to treatment groups based on their tumor sizes; tumor size is measured in 2 dimensions using a caliper, and the volume is expressed in mm3 using the formula: V = 0.5 a × b2 where a and b are the long and short diameters of the tumor, respectively. Pretreatment randomization ensures that each group has approximately the same mean tumor size. Mice are treated with vehicle (5% dextrose), SGI-1776 or cytarabine (ara-C). SGI-1776 and ara-C are formulated in 5% dextrose. SGI-1776 is administered by oral gavage (PO) on a daily × 5/week or twice/week schedule; ara-C is administered by intraperitoneal injection 3 times/week for 3 consecutive weeks. Animals are euthanized when their measured tumor size is greater than 3000 mm3 or when they lose ≥ 20% initial body weight; if the body weight loss ≥ 15%, treatment is stopped at first until mice regain body weight. Mice are euthanized when body weight loss is still ≥ 20% even after stopping treatment. T/C value (in %) is an indication of antitumor efficacy, where T and C are the mean tumor volume of the treated and control groups, respectively, on a given day. The differences between the mean tumor sizes for comparing groups is analyzed using the ANOVA test, where P ≤ 0.05 is considered to be statistically significant.

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

    参考文献

    SGI-1776 free base 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 2.4666 mL 12.3329 mL 24.6658 mL 61.6644 mL
    5 mM 0.4933 mL 2.4666 mL 4.9332 mL 12.3329 mL
    10 mM 0.2467 mL 1.2333 mL 2.4666 mL 6.1664 mL
    15 mM 0.1644 mL 0.8222 mL 1.6444 mL 4.1110 mL
    20 mM 0.1233 mL 0.6166 mL 1.2333 mL 3.0832 mL
    25 mM 0.0987 mL 0.4933 mL 0.9866 mL 2.4666 mL
    30 mM 0.0822 mL 0.4111 mL 0.8222 mL 2.0555 mL
    40 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5416 mL
    50 mM 0.0493 mL 0.2467 mL 0.4933 mL 1.2333 mL
    60 mM 0.0411 mL 0.2055 mL 0.4111 mL 1.0277 mL
    80 mM 0.0308 mL 0.1542 mL 0.3083 mL 0.7708 mL
    100 mM 0.0247 mL 0.1233 mL 0.2467 mL 0.6166 mL
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