1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. (±)-Zanubrutinib

(±)-Zanubrutinib (Synonyms: (±)-BGB-3111)

目录号: HY-101474 纯度: 99.73%
产品使用指南

(±)-Zanubrutinib ((±)-BGB-3111) 是一种有效选择性的,具有口服活性的 Bruton's 酪氨酸激酶 (Btk) 抑制剂。

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(±)-Zanubrutinib Chemical Structure

(±)-Zanubrutinib Chemical Structure

CAS No. : 1633350-06-7

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1452
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5 mg ¥1400
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10 mg ¥2750
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50 mg ¥7000
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Other Forms of (±)-Zanubrutinib:

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Top Publications Citing Use of Products

    (±)-Zanubrutinib purchased from MCE. Usage Cited in: Dr. Wang from Chinese Academy of Sciences.

    Determining IC50 for Zanubrutinib. IC50 values for Zanubrutinib are determined using the ADP-Glo Kinase Assay. Curve fitting is performed using GraphPad Prism sigmoidal dose-response (variable slope) software.

    (±)-Zanubrutinib purchased from MCE. Usage Cited in: Dr. Wang from Chinese Academy of Sciences.

    Determining IC50 for Zanubrutinib. IC50 values for Zanubrutinib are determined using the ADP-Glo Kinase Assay. Curve fitting is performed using GraphPad Prism sigmoidal dose-response (variable slope) software.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    (±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor[1].

    体外研究
    (In Vitro)

    In both biochemical and cellular assays, (±)-Zanubrutinib ((±)-BGB-3111) demonstrates nanomolar Btk inhibition activity. In several MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with PCI-32765, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK[1].

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

    体内研究
    (In Vivo)

    (±)-Zanubrutinib induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts. Preliminary 14-day toxicity study in rats shows that (±)-Zanubrutinib is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250mg/kg/day[1].

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

    分子量

    471.55

    Formula

    C27H29N5O3

    CAS 号
    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 30 mg/mL (63.62 mM)

    Ethanol : ≥ 10 mg/mL (21.21 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1207 mL 10.6033 mL 21.2067 mL
    5 mM 0.4241 mL 2.1207 mL 4.2413 mL
    10 mM 0.2121 mL 1.0603 mL 2.1207 mL
    *

    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。-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。

    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

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.41 mM,饱和度未知) 的澄清溶液。

      以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (4.41 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.08 mg/mL (4.41 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 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。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.41 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 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玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    纯度: 99.73%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    (±)-Zanubrutinib
    目录号:
    HY-101474
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