HRK Factory Cladribine Raw Materials Powder on sale

CAS:4291-63-8

MF:C11H15ClN2O5

MW:290.7

EINECS:200-184-4

Specification​: 99% min Cladribine Powder

Sample:Cladribine Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:white

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Cladribine Usage and Function.

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.

Cladribine injection is primarily used to interfere with the treatment of active anemia with clinical significance after treatment failure, as well as thrombocytopenia, neutropenia, and disease-associated hair-cell leukemia. This product is a prescription drug and should be used under the guidance of a doctor. The main ingredient of this product is clatribine. The character of this product is colorless or almost colorless clear liquid, if the drug is found to have changed during the drug use, it should be prohibited.

In vitro study of Cladribine.

Cladribine exerts remarkable activity against hair-cell leukemia (HCL), a chronic B-lymphocytic hyperplasia disease, prolongating complete remission. Cladribine induces the accumulation of DNA strand breaks and subsequently activates the tumor suppressor gene p53 in lymphocytes. Cladribine may regulate STAT3 activity in MM cells. Cladribine inhibited proliferation/survival of U266, RPMI8226 and MM1.S cells in a dose-dependent manner. U266 had the lowest sensitivity to cladribine and the highest sensitivity to MM1.S. Treatment with Cladribine gradually increased the proportion of G1 phase cells in the cell cycle and decreased S phase cells. Treatment with Cladribine for 24 hours appeared to increase the proportion of G2-M phase in U266 cells. A dose-dependent increase in apoptosis induced by cladribine was observed in both RPMI8226 and MM1.S cells. Time-dependent treatment with 0.2 μM cladribine significantly induced caspase-3, -8, and -9 activation and PARP cleavage in MM1.S. Cladribine significantly reduced phosphate STAT3 (P-STAT3) levels in a dose-dependent manner, but did not affect total STAT3 protein levels. Cladribine has the potential to induce apoptosis in HSB2 cells in a concentration-dependent manner. Cladribine inhibited primary mast cell (MC) and MC line HMC-1 growth in a dose-dependent manner, and HMC-1.2 cells containing KIT D816V had lower IC50 values compared to HMC-1.1 cells lacking KIT D816V.

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).