Overview
Dasatinib is a second-generation tyrosine kinase inhibitor (TKI) developed for targeted cancer therapy. It was approved by the FDA in 2006 for treating chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Compared to first-generation TKIs like imatinib, dasatinib exhibits higher potency and broader kinase inhibition, particularly against BCR-ABL and SRC family kinases. As a small molecule drug, dasatinib works by binding to the ATP-binding site of target kinases, blocking their activity and inhibiting uncontrolled cell proliferation. Its clinical success has made it a critical component in hematologic malignancy treatment protocols worldwide.
Physical and Chemical Properties
Dasatinib appears as a white to off-white crystalline powder with a molecular weight of 488.01 g/mol. The compound shows good solubility in dimethyl sulfoxide (DMSO) but limited solubility in aqueous solutions, which influences its pharmaceutical formulation strategies. Chemically, dasatinib features a thiazole-carboxamide core structure with chlorine and methyl substitutions, contributing to its selective kinase binding affinity. The molecule's stability is maintained under recommended storage conditions (2-8°C), though it may degrade when exposed to moisture or prolonged light exposure.
Main Applications
The primary medical application of dasatinib is the treatment of Philadelphia chromosome-positive leukemias. It serves as first-line therapy for chronic-phase CML and salvage therapy for imatinib-resistant cases. The drug is also indicated for Ph+ ALL and has shown efficacy in certain solid tumor research models. Beyond oncology, dasatinib has been investigated for potential applications in pulmonary arterial hypertension and fibrotic disorders due to its PDGFR inhibition properties. However, these off-label uses remain experimental and require further clinical validation.
Safety and Storage
As a potent bioactive compound, dasatinib requires careful handling in laboratory and industrial settings. Personal protective equipment including gloves and safety goggles should be worn to prevent skin contact or inhalation of powder particles. Proper storage involves maintaining the substance in tightly sealed containers under refrigerated conditions (2-8°C) with desiccant packs to prevent moisture absorption. Bulk quantities should be segregated in dedicated pharmaceutical storage areas with controlled access. Shelf life typically extends 24-36 months when stored correctly.
B2B Procurement Guide
Pharmaceutical manufacturers and research institutions sourcing dasatinib should prioritize suppliers with GMP certification and verifiable track records. Key procurement considerations include batch-specific Certificate of Analysis (COA) documentation confirming identity (HPLC, NMR), purity (≥98%), and absence of heavy metal contaminants. For clinical-grade material, regulatory documentation including Drug Master Files (DMF) and suitability for formulation processes should be verified. Market prices fluctuate based on quantity (gram to kilogram scale) and purity specifications, with research-grade material typically priced lower than pharmacopeia-grade API.
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