1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  2. JAK
  3. AZD-1480

AZD-1480 是一种 ATP 竞争型的 JAK1JAK2 抑制剂,IC50 分别为 1.3 nM 和 0.4 nM。

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AZD-1480 Chemical Structure

AZD-1480 Chemical Structure

CAS No. : 935666-88-9

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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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5 mg ¥800
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10 mg ¥1252
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50 mg ¥3800
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100 mg ¥6428
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Customer Review

Other Forms of AZD-1480:

    AZD-1480 purchased from MCE. Usage Cited in: Clin Cancer Res. 2018 Apr 15;24(8):1917-1931.  [Abstract]

    Jak2 is inhibited by lentiviral expression of Jak2 shRNA or control shRNA in CWR22Pc and CWR22Rv1 cells. Alternatively, cells are treated with Jak2 inhibitors AZD1480 (0.8 μM) and INCB018424 (0.4 μM) (72 h), followed by Western blot analysis of Jak2 and active Stat5a/b.

    AZD-1480 purchased from MCE. Usage Cited in: Neuro Oncol. 2017 Jan;19(1):22-30.  [Abstract]

    AZD1480 and RXDX-101 decrease pSTAT3 levels in a dose- and time-dependent manner. (A) Ink4a-/-/Arf-/-/NTRK2-TEL astrocytes are treated with different concentrations of AZD1480 (upper panel) or RXDX-101 (lower panel) for 1 h. (B) Cells are treated with 0.5 μM AZD1480 (upper panel) or 0.05 μM RXDX-101 (lower panel) for the indicated times. Western blot analyses are then performed with the indicated antibodies.

    AZD-1480 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2017 Nov;95:1799-1808.  [Abstract]

    The expression of Bcl-2, Bax, pro-Caspase-3 and cleaved-Caspase-3 by western blotting. Representative western blots showing the effects of apigenin and AZD1480 on Bax, Bcl-2, pro-Caspase-3 and cleaved-Caspase-3 expression levels.

    查看 JAK 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

    AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively[1].

    IC50 & Target[1]

    JAK2

    <0.4 nM (IC50)

    JAK1

    1.3 nM (IC50)

    体外研究
    (In Vitro)

    AZD-1480 (5 μM) 通过抑制 Aurora 激酶诱导 G2/M 停滞和细胞死亡[1]
    AZD-1480 是一种有效的 JAK2 抑制剂,可以抑制生长、存活以及作为 FGFR3STAT3 信号和下游靶点,包括人多发性骨髓瘤细胞中的细胞周期蛋白 D2。在低微摩尔浓度下,AZD-1480 可阻断细胞增殖并诱导骨髓瘤细胞系凋亡[2]
    AZD-1480 可有效阻断组成型和刺激诱导的 JAK1、JAK2 和 STAT- 3 在人和小鼠神经胶质瘤细胞中的磷酸化,并导致细胞增殖减少和细胞凋亡的诱导[3]
    AZD-1480 是一种有效的竞争性小分子抑制剂JAK1/2 激酶,并且它能够以 STAT3 依赖性方式抑制 STAT3 磷酸化和肿瘤生长。AZD-1480 部分通过影响肿瘤微环境来抑制肿瘤血管生成和转移[4]

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

    体内研究
    (In Vivo)

    AZD-1480 抑制人实体瘤和多发性骨髓瘤异种移植模型中的 STAT3 磷酸化[1]
    在体内,AZD-1480 抑制皮下肿瘤的生长并提高小鼠的存活率通过抑制 STAT-3 活性来抑制颅内胶质母细胞瘤 (GBM) 肿瘤,表明 AZD-1480 对 JAK/STAT-3 通路的药理学抑制应考虑用于处理 GBM 肿瘤患者的研究[3]
    AZD-1480 在小鼠同源实验模型和自发转移模型中阻断骨髓细胞的肺浸润和肺转移的形成。此外,AZD-1480 减少人异种移植肿瘤模型中的血管生成和转移[4]
    AZD-1480 抑制具有持续 Stat3 活性的人实体瘤异种移植物的生长[5]

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

    Clinical Trial
    分子量

    348.77

    Formula

    C14H14ClFN8

    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
    细胞实验: 

    DMSO 中的溶解度 : 50 mg/mL (143.36 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 2.8672 mL 14.3361 mL 28.6722 mL
    5 mM 0.5734 mL 2.8672 mL 5.7344 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

    动物实验:

    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 (7.17 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.17 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 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: 99.91%

    参考文献
    Kinase Assay
    [5]

    Inhibition studies of AZD1480 are performed using recombinant Jak1, Jak2, or Jak3 under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 mM/mL BSA, and 10 mM MgCl2. Jak3 enzyme is expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes are assayed in the presence of AZD1480 (10 point dose response, in triplicate, from 8.3 μM to 0.3 nM in half-log dilution steps) using 1.5 μM peptide substrate (Jak1: FITC-C6-KKHTDDGYMPMSPGVA-NH2, Jak2 and Jak3: FAM-SRCtide) and screened under their respective ATP Km (Jak1: 55 μM, Jak2: 15 μM, Jak3: 3 μM) and approximated physiological ATP concentration of 5 mM. Phosphorylated and unphosphorylated peptides are separated and quantified by a Caliper LC3000 system for calculating percent inhibition.

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

    Cell Assay
    [4]

    Renca or 786-O cells are suspended in DMEM medium with 5% FBS, and seeded in 96-well plates (5×103 per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 hours. Cell viability is determined by MTS assay. Absorbance at 490 nm is measured with Mikrotek Laborsysteme. Mouse endothelial cells and splenic CD11b+/c- myeloid cells are enriched from tumor-bearing mice,and cultured in 5% FBS RPMI-1640 medium. HUVECs are cultured on collagen 1-coated plates in complete medium. All cells are treated with DMSO and AZD1480 at various doses for 24 hours. Cell viability is determined by counting cell number manually. All the experiments are repeated 3 times.

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

    Animal Administration
    [1]

    For subcutaneous (s.c.) tumor model, 2.5×106 Renca or 786-O cells suspended in 100 μL PBS are injected into the flank of BALB/c or nude mice, respectively. When average tumor volume reaches approximately 100-150 mm3, AZD1480 or vehicle is administered by oral gavage either once a day at the dose of 50 mg/kg, or twice daily at 30 mg/kg, as indicated. Tumor size is measured by caliper every other day. For experimental lung metastasis model, 0.1×106 Renca or 1×106 786-O cells suspended in 500 μL PBS are injected via tail vein to BALB/c or nude mice, respectively. Three days later, mice are orally treated with AZD1480 (50 mg/kg/d) or vehicle for 21 days for Renca tumors and 60 days for 786-O tumors respectively. For the Calu-6 model, 3×106 tumor cells in matrigel are implanted s.c. into the flanks of nude mice, randomized into vehicle (twice daily, BID) and drug treatment (AZD1480, 30 mg/kg BID) groups, and dosed orally daily for 19 days. For spontaneous lung metastasis model, 2×105 4T1 cells suspended in 100 μL PBS are injected in the mammary gland of female BALB/c mice by gently penetrating the skin. AZD1480 (50 mg/kg/d) or vehicle is given orally for 21 days.

    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, 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 2.8672 mL 14.3361 mL 28.6722 mL 71.6805 mL
    5 mM 0.5734 mL 2.8672 mL 5.7344 mL 14.3361 mL
    10 mM 0.2867 mL 1.4336 mL 2.8672 mL 7.1680 mL
    15 mM 0.1911 mL 0.9557 mL 1.9115 mL 4.7787 mL
    20 mM 0.1434 mL 0.7168 mL 1.4336 mL 3.5840 mL
    25 mM 0.1147 mL 0.5734 mL 1.1469 mL 2.8672 mL
    30 mM 0.0956 mL 0.4779 mL 0.9557 mL 2.3893 mL
    40 mM 0.0717 mL 0.3584 mL 0.7168 mL 1.7920 mL
    50 mM 0.0573 mL 0.2867 mL 0.5734 mL 1.4336 mL
    60 mM 0.0478 mL 0.2389 mL 0.4779 mL 1.1947 mL
    80 mM 0.0358 mL 0.1792 mL 0.3584 mL 0.8960 mL
    100 mM 0.0287 mL 0.1434 mL 0.2867 mL 0.7168 mL
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    产品名称:
    AZD-1480
    目录号:
    HY-10193
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