1. Metabolic Enzyme/Protease Apoptosis
  2. Adenosine Deaminase Apoptosis
  3. Cladribine

Cladribine  (Synonyms: 克拉屈滨; 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA)

目录号: HY-13599 纯度: 99.97%
COA 产品使用指南

Cladribine (2-Chloro-2′-deoxyadenosine) 是一种嘌呤核苷类似物,是具有口服活性的腺苷脱氨酶 (adenosine deaminase) 抑制剂。Cladribine 能作为 DNA 合成 (DNA synthesis) 的抑制剂,可阻断受损 DNA 的修复。Cladribine 可以抑制 DNA 甲基化。Cladribine 具有抗淋巴瘤活性,可用于一些血液恶性肿瘤和多发性硬化的研究。

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Cladribine Chemical Structure

Cladribine Chemical Structure

CAS No. : 4291-63-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥500
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5 mg ¥233
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10 mg ¥350
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50 mg ¥1245
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100 mg ¥2115
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500 mg   询价  

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Customer Review

    Cladribine purchased from MCE. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.  [Abstract]

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with Cladribine, Dasatinib or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis[1][2].

    IC50 & Target

    Adenosine deaminase[2]

    体外研究
    (In Vitro)

    Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation[1].
    ? Cladribine (1-4 μM; 24 hours) induces G1 phase arrest via decreasing the expressions of Cyclin D1 and Cyclin E, and increasing the expressions of p21 and p27 in DLBCL cells[1].
    ? Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells[1].
    ? Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress[1].
    ? Cladribine inhibits cell proliferation of multiple myeloma (MM) cells in a dose-dependent manner; with IC50s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively[2].

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

    Cell Proliferation Assay[1]

    Cell Line: The human DLBCL cell lines (U2932, OCI-LY10, SUDHL2, WSU-DLCL2, DB)
    Concentration: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours, 48 hours
    Result: Exhibited notable suppression of cell proliferation in five DLBCL cells.

    Western Blot Analysis[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Decreased the expressions of Cyclin D1 and Cyclin E, and increased the expressions of p21 and p27.

    Apoptosis Analysis[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Induced apoptosis and activates exogenous and endogenous apoptotic signaling pathways.

    Cell Cycle Analysis[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Caused G1 phase arrest.

    RT-PCR[1]

    Cell Line: U2932 cells, WSU-DLCL2 cells
    Concentration: 0 μM, 1 μM, 2 μM, 4 μM
    Incubation Time: 24 hours
    Result: Activated ER stress.
    体内研究
    (In Vivo)

    Cladribine (10 μg/kg; i.p.; 3 times/week; for 2 weeks) may have benefits in the treatment of ischemia/reperfusion injury to the biochemical and histopathologic parameters[3].
    ? Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice[4].
    ? Cladribine exhibits Cmax (rat 4.9 ng/mL) following intra-arterial injection[5].
    ? Cladribine exhibits Cmax (rat 1.1 ng/mL) following subcutaneous injection[5].
    ? Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection[5].
    ? Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection[5].
    ? Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose[5].

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

    Animal Model: Male Sprague-Dawley rats, ischemic injury model[3]
    Dosage: 10 μg/kg
    Administration: Intraperitoneal injection, 3 times/week, for 2 weeks
    Result: Might increase expression of Sphk1 and consecutively SphK1 suppressed HIF-1α.
    Animal Model: Male Sprague Dawley rats (350-450 g)[5]
    Dosage: 2 mg/kg for s.c., 1 mg/kg for i.a. (Pharmacokinetic Analysis)
    Administration: Subcutaneous injection, intra-arterial
    Result: Cmax (4.9 ng/mL i.a.; 1.1 ng/mL s.c.), T1/2 β (3.5 h i.a.; 4.5 s.c.).
    Clinical Trial
    分子量

    285.69

    Formula

    C10H12ClN5O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    克拉屈滨

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 30 mg/mL (105.01 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 10 mg/mL (35.00 mM; 超声助溶)

    * "≥" 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 3.5003 mL 17.5015 mL 35.0030 mL
    5 mM 0.7001 mL 3.5003 mL 7.0006 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 year; -20°C, 6 months (protect from light)。-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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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:

    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: PBS

      Solubility: 25 mg/mL (87.51 mM); 澄清溶液; 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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.97%

    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 year; -20°C, 6 months (protect from light)。-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
    H2O / DMSO 1 mM 3.5003 mL 17.5015 mL 35.0030 mL 87.5074 mL
    5 mM 0.7001 mL 3.5003 mL 7.0006 mL 17.5015 mL
    10 mM 0.3500 mL 1.7501 mL 3.5003 mL 8.7507 mL
    15 mM 0.2334 mL 1.1668 mL 2.3335 mL 5.8338 mL
    20 mM 0.1750 mL 0.8751 mL 1.7501 mL 4.3754 mL
    25 mM 0.1400 mL 0.7001 mL 1.4001 mL 3.5003 mL
    30 mM 0.1167 mL 0.5834 mL 1.1668 mL 2.9169 mL
    DMSO 40 mM 0.0875 mL 0.4375 mL 0.8751 mL 2.1877 mL
    50 mM 0.0700 mL 0.3500 mL 0.7001 mL 1.7501 mL
    60 mM 0.0583 mL 0.2917 mL 0.5834 mL 1.4585 mL
    80 mM 0.0438 mL 0.2188 mL 0.4375 mL 1.0938 mL
    100 mM 0.0350 mL 0.1750 mL 0.3500 mL 0.8751 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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:
    Cladribine
    目录号:
    HY-13599
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