Supply Cladribine Raw Materials powder

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Clatribine is a halogenated derivative of deoxyadenosine, and its phosphorylated derivative can cause DNA breakage, enhance the effect of endogenous dATP on apoptotic bodies, and cause mitochondrial toxicity, leading to cell apoptosis. This product can inhibit DNA synthesis and repair in lymphocyte and monocyte in differentiation or resting stage.

Clatribine is the first-line drug for the treatment of hairy cell leukemia, and a high complete remission rate can be achieved after a single course of clatribine monotherapy

Cladribine is an effective antitumor drug, but also has serious potential side effects, such as hematological toxicity, can cause anemia, leukopenia, thrombocytopenia, liver toxicity, infection, etc. Therefore, blood routine, bone marrow and liver and kidney function should be tested regularly during and after treatment.

Uses of Cladribine.

In vivo study of Cladribine.

Cladribine(0.7-3.5mM) and/or diltiazem(2.4mM), intraperitoneically injected into adult zebrafish, were analyzed by HPLC for levels of purine nucleotides, red blood cell (RBC) lysates, such as ATP, a potential marker of cardiovascular health.​ After the administration of Ia and s.c., the plasma concentration of Cladribine decreased rapidly with biphasic decline. A single dose of Cladribine is 1mg/kgia and 2mg/kgs.c. After injection, AUC and t1/2β were 0.66:1.2μg×h/mL and 3.5:4.5 h, respectively.

Product method of Bulk Cladribine Powder.

2, 6-dichloropurine (I)(0.95g, 5mmo1) and sodium hydride (50% dispersed oil, 0.25g, 5.2mmo1) were suspended in 35ml anhydrous acetonitrile and stirred at room temperature and under nitrogen protection for 30min. 1-chloro-2-deoxy-3, 5-di-O-p-toluenyl-α-D-erythrace-pentose (II)(1.95g, 5mmo1) was added in batches within 20min under stirring. Add it and stir for another 15h. Filter out a small amount of insoluble matter and concentrate the filtrate. The remaining oil was eluted by silica gel column chromatography with toluene-acetone (9:1, volume ratio). The obtained solid was then crystallized with ethanol to obtain 1.60g compound (Ⅲ) with a yield of 59% and a melting point of 159-162℃. Compound (Ⅲ)(2.50g, 4.6mmo1) was dissolved in 60ml methanol solution saturated with ammonia (0℃ saturation) and stirred at 100℃ for 5h. The residue was then eluted with chloroform-methanol (8:2, volume ratio) by silica gel column chromatography. Then ethanol was crystallized to obtain 0.87g clatrobine with 71% yield and melting point 220℃(softened).

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