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Cladribine
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品牌名称:$brandModel.Title(进口品牌)型号: 原产地:美洲 发布时间:2021/7/26更新时间:2024/1/2
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Cladribine
CAS No. : 4291-63-8
MCE 站:Cladribine
产品活性: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。
研究领域:Metabolic Enzyme/Protease | Apoptosis
作用靶点:Adenosine Deaminase | Apoptosis
In Vitro: Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation.
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.
Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells.
Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress.
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.
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.
Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice.
Cladribine exhibits Cmax (rat 4.9 ng/mL) following intra-arterial injection.
Cladribine exhibits Cmax (rat 1.1 ng/mL) following subcutaneous injection.
Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection.
Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection.
Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose.
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