China Factory Supply Cladribine Powder CAS 4291-63-8 Raw Material

CAS:  4291-63-8

MF: C10H12ClN5O3

MW:285.69

EINECS: 636-978-6

Specification​: 99% min Cladribine 

Sample:  Cladribine Powder

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Portal:https://henrikang.en.made-in-china.com/

Cladribine Powder Usage and Synthesis.

Cladribine Powder is primarily effective in hairy cell leukemia, but also in other lymphomas and leukemias. Cladribine Raw Material exerts significant activity in hairy cell leukemia (HCL), a chronic B-lymphoproliferative disease, extending the period of complete remission. CAS No. 4291-63-8, Molecular Formula C10H12ClN5O3, Molecular Weight 285.69, EINECS No. 636-978-6.

Crystallized from water, softened at 210-215°C, cured and turned brown; crystallized from ethanol, melting point 22023 (softened), then cured and turned brown, no longer melted at <300°C. [α]D23-18.8° (C=1, dimethylformamide). UV maximum absorption (0.1 mol/L sodium hydroxide): 265nm: (0.1 mol/L hydrochloric acid): 265nm.

Cladribine, the name of Western medicine. Commonly used dosage form is injection. Cladribine Raw Material is used for the treatment of hairy cell leukemia (HCL) with clinically significant anemia, neutropenia, thrombocytopenia, and disease-related symptoms that are active after failure of interferon therapy.

The main effect of Cladribine Injection is blood activation and hematopoiesis, which can be generally used for the treatment of leukemia and neutropenia, and is very effective in the treatment of anemia symptoms such as weakness, limb weakness and facial atrophy. Cladribine injection is a colorless clarified liquid, the main ingredient is cladribine and the excipient is sodium chloride. Very few patients may experience mild symptoms such as nausea, headache, pain at the injection site, fatigue, etc., which will subside on their own after discontinuation of the drug.

Application/Function of Cladribine Powder.

The tumor suppressive effect of cladribine is related to the activity of deoxycytidine kinase and deoxyribonucleotide kinase. Cladribine enters the cell by passive transport and is phosphorylated into cladribine triphosphate, which is incorporated into DNA molecules and prevents DNA repair after breakage, resulting in disruption of cellular metabolism and affecting cellular DNA synthesis.

Therefore, cladribine inhibits DNA synthesis and repair in differentiated or quiescent lymphocytes and monocytes. Cladribine Powder is used clinically for the treatment of active hairy cell leukemia with clinically significant anemia, neutropenia, thrombocytopenia, and disease-related symptoms after failure of interferon therapy.

Cladribine Powder is a halogenated derivative of deoxyadenosine, whose phosphorylated derivative triggers DNA breaks, enhances the action of endogenous dATP on apoptotic bodies, as well as being toxic to mitochondria, leading to apoptosis.Cladribine Raw Material has been shown to inhibit DNA synthesis and repair.

Cladribine Raw Material is the first-line drug for the treatment of hairy cell leukemia, and a high rate of complete remission can be achieved with a single course of cladribine monotherapy.

Cladribine Powder is an effective antitumor agent, but also has serious potential toxicities, such as hematologic toxicity, which can cause anemia, leukopenia, thrombocytopenia, hepatotoxicity, and infection. Therefore, routine blood, bone marrow and liver and kidney functions should be tested regularly during and after treatment.

Pharmacological Effects of Cladribine Powder

• 1. The interaction of cladribine with other drugs is not known.
• 2. The toxicity of Cladribine Powder may be exacerbated by the concomitant use of drugs that impair bone marrow hematopoiesis, immune function, and renal function during the administration of this product.

The tumor-suppressive activity of cladribine is related to the activity of deoxycytidine kinase and deoxynucleotide kinase. It enters the cell mainly by passive transport, is phosphorylated by deoxycytidine kinase in the cell and converted into cladribine triphosphate, which is incorporated into the DNA molecule, impeding the repair of DNA after breakage, causing depletion of NAD and ATP, disrupting cellular metabolism, and affecting cellular DNA synthesis. Therefore, this product has an inhibitory effect on DNA synthesis and repair in differentiated or quiescent lymphocytes and monocytes.

Production method of 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 for 30min at room temperature under nitrogen protection. 1-chloro-2-deoxy-3,5-dio-O-p-toluoyl-α-D-erythro-pentofuranose (II) was added in batches within 20min under stirring. ) (1.95 g, 5 mmo1). After addition, the mixture was stirred for another 15 h. A small amount of insoluble material was filtered off and the filtrate was concentrated. The remaining oily material was subjected to silica gel column chromatography and eluted with toluene-acetone (9:1, v/v).

The solid obtained was then crystallized in ethanol to give 1.60 g of compound (III) in 59% yield with a melting point of 159-162°C. Compound (III) (2.50 g, 4.6 mmo1) was dissolved in 60 ml of saturated ammonia in methanol solution (saturated at 0 °C) and stirred at 100 °C for 5 h. Evaporated to dryness and the residue was subjected to silica gel column chromatography and eluted with chloroform-methanol (8:2, v/v). Then ethanol crystallized to give 0.87g of cladribine in 71% yield with a melting point of 220°C (softening).