产品
编 号：F356331
分子式：C10H12ClN5O3
分子量：285.69
分子式：C10H12ClN5O3
分子量：285.69
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
187
In-stock
10mg
280
In-stock
50mg
996
In-stock
100mg
1692
In-stock
结构图
CAS No: 4291-63-8
产品详情
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.
体内研究：
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.Animal Model:Male Sprague-Dawley rats, ischemic injury model
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)
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.).
体外研究：
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.
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.
体内研究：
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.Animal Model:Male Sprague-Dawley rats, ischemic injury model
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)
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.).
体外研究：
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.
产品资料
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