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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 C_max (rat 4.9 ng/mL) following intra-arterial injection.
Cladribine exhibits C_max (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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