1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
  3. Bemcentinib

Bemcentinib  (Synonyms: R428; BGB324)

目录号: HY-15150 纯度: 99.95%
COA 产品使用指南

Bemcentinib (R428) 是一种选择性的、具有口服活性的 Axl 抑制剂,IC50 值为 14 nM。

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Bemcentinib Chemical Structure

Bemcentinib Chemical Structure

CAS No. : 1037624-75-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1560
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2 mg ¥779
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5 mg ¥1400
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10 mg ¥2438
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50 mg ¥4700
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100 mg ¥7400
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Other Forms of Bemcentinib:

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 37 篇科研文献

WB

    Bemcentinib purchased from MCE. Usage Cited in: Mil Med Res. 2023 Feb 22;10(1):7.  [Abstract]

    Bemcentinib (BGB324; 1 μM; 30 min) partially blocks the activation of HSC by rGAS6 in LX-2 cells.

    Bemcentinib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.  [Abstract]

    Western blot showing PKCδ expression in nuclear extracts of GR4 and GR10 cells treated with 1 μM gef in combination with 2.5 μM R428 and 5 μM GW572016 (Lapa) for 24 hr.

    Bemcentinib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4.  [Abstract]

    Western blot showing phosphorylated PLCγ2 in cells treated with gef (1 μM) and R428 or Lapa for 24 hr. SE, short exposure; LE, long exposure.

    Bemcentinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Bemcentinib purchased from MCE. Usage Cited in: Sci Rep. 2017 Dec 19;7(1):17770.  [Abstract]

    Western blot analysis of pAXL level in H1299 cells treated with the indicated concentration of R428 for 1 h. Results are confirmed in three independent experiments.

    Bemcentinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 20;8(25):41064-41077.  [Abstract]

    The expression of AXL in the PC3-DR and DU145-DR cells treated with R428 (1 μM) is analyzed by western blotting.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM[2].

    IC50 & Target

    IC50: 14 nM (Axl kinase)[1][2].

    体外研究
    (In Vitro)

    Bemcentinib (R428) (2 μM) 显著干扰Axlpos黑色素瘤细胞的迁移和侵袭机制,其水平与Axl敲低相当[1]。bmcentinib (R428)协同CDDP增强肝脏微转移抑制作用[2]
    bmcentinib (R428) (50 nM-1 μM)可引起前脂肪细胞向成熟脂肪细胞分化的浓度依赖性抑制,这可以通过降低脂质摄取得到证明[3]

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

    体内研究
    (In Vivo)

    Bemcentinib (R428) (125 mg/kg, p.o.) 显著阻断MDA-MB-231-luc-D3H2LN在两种独立小鼠乳腺癌扩散模型中的转移发展,抑制肿瘤血管生成和血管内皮生长因子(VEGF)诱导的角膜新生血管生成[2].
    Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) 让老鼠保持高脂肪饮食导致体重增加和皮下和性腺脂肪量显著减少[3]

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

    Clinical Trial
    分子量

    506.64

    Formula

    C30H34N8

    CAS 号
    性状

    固体

    颜色

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

    DMSO 中的溶解度 : 25 mg/mL (49.34 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 1.9738 mL 9.8689 mL 19.7379 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 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。-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% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.11 mM); 悬浊液; 超声助溶

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

      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/saline water

      Solubility: 12.5 mg/mL (24.67 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂: 0.5%HPMC  1%Tween80

      Solubility: 5 mg/mL (9.87 mM); 悬浊液; 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: 99.95%

    参考文献
    Cell Assay
    [1]

    Cells maintained for 24 hours in serum-free medium are harvested and transferred to the upper chamber (1.5×105 cells per well) of uncoated (migration) or matrigel-coated (invasion) 24-well chambers. RPMI medium containing 10% fetal bovine serum is added to the lower chamber. Bemcentinib (R428) (2 μM) or vehicle (DMSO, 0.25%) is added for 2 hours to cells before loading them in the upper chambers. Both the upper and lower chambers contain the drug or vehicle. Quantification of migrating/invading cells is obtained by measuring their fluorescent signals with a 480/520 nm filter set on an Infinite M1000 microplate reader 20 or 42 hours later, respectively.

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

    Animal Administration
    [2]

    Seven- to 8-wk-old female NCr nu/nu mice are injected intracardially with bioluminescent MDA-MB-231-luc-D3H2LN cell suspension. Oral dosing with Bemcentinib (R428) (125 mg/kg, p.o.) or vehicle twice daily begins 2 h before cell implantation and continue to day 21 (n=20). Metastatic burden is quantified by in vivo bioluminescence imaging on day 22 and analyzed using the Wilcoxon rank sum test.

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

    参考文献

    Bemcentinib 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, 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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9738 mL 9.8689 mL 19.7379 mL 49.3447 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL 9.8689 mL
    10 mM 0.1974 mL 0.9869 mL 1.9738 mL 4.9345 mL
    15 mM 0.1316 mL 0.6579 mL 1.3159 mL 3.2896 mL
    20 mM 0.0987 mL 0.4934 mL 0.9869 mL 2.4672 mL
    25 mM 0.0790 mL 0.3948 mL 0.7895 mL 1.9738 mL
    30 mM 0.0658 mL 0.3290 mL 0.6579 mL 1.6448 mL
    40 mM 0.0493 mL 0.2467 mL 0.4934 mL 1.2336 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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