Dasatinib Chemical Properties

Melting point 275-286°C

density 1.408±0.06 g/cm3(Predicted)

storage temp. -20°C Freezer

form White powder.

pka 10.94±0.70(Predicted)

CAS DataBase Reference 302962-49-8(CAS DataBase Reference)

Safety Information

HS Code 29341000

MSDS Information

Dasatinib Usage And Synthesis

Leukemia drug Dasatinib is an oral potent oncogenic kinase inhibitor, which can block signal of cancer cell replication acceleration , in May 2009, the US Food and Drug Administration (FDA) formally approved the sale of dasatinib , It has been clinically used for the treatment of various chronic myeloid leukemia (CML), including treatment of chronic myeloid leukemia which is resistant or intolerant to the treating programs including imatinib mesylate., Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph + ALL) and the treatment of patients with solid tumors.

October 28, 2010 ,the FDA approved dasatinib (Sprycel) of the new indication which is used for the treatment of the rare leukemia first diagnosed Philadelphia chromosome-positive called chronic myeloid leukemia (Ph + CP-CML) . The disease is a blood and bone marrow disease associated with genetic abnormality .

An open-label randomized clinical trial conducted in patients with CP-CML evaluated the safety and efficacy of dasatinib . Common side effects include decreased activity of the bone marrow caused by red blood cells, white blood cells and platelets decreased (myelosuppression), fluid retention, diarrhea, headache, musculoskeletal pain, and rash.

October 11, 2011, the US Food and Drug Administration (FDA) said the leukemia drug dasatinib (Sprycel, Bristol-Myers Squibb Company) might increase pulmonary arterial hypertension (PAH) risk. Pulmonary hypertension is a rare but serious disease that can lead to the condition that heart pumping blood to the lungs becomes more difficult by raising the pressure . PAH symptoms include shortness of breath, fatigue, swelling of the legs and ankles, clinicians must differentiate these symptoms from other similar symptoms.

Since 2006 Dasatinib was approved in the US market ,there had been 12 associated pulmonary hypertension events ,pulmonary hypertension symptoms included shortness of breath, fatigue, hypoxia and fluid retention, patients then were confirmed pulmonary hypertension by the results of right heart catheterization ,studies have shown that the biggest cause of the disease may come from patients taking dasatinib.

The above information is edited by the Chemicalbook of Tian Ye.

Chemical properties White solid

Uses Suitable for treatment of chronic myeloid leukemia which is resistant or intolerant to the treating programs including imatinib mesylate.

Description Chronic myeloid leukemia (CML), a hematological stem-cell disorder, is definitively diagnosed by the detection of the Philadelphia chromosome, a truncated version of chromosome 22 resulting from the reciprocal translocation of chromosomes 9 and 22 induced by a single mutagenic event. The consequence is the juxtaposition of two genes creating a fusion gene BCR-ABL. This gene translates a fusion protein with increased tyrosine kinase activity that contributes to the pathogenesis of CML. Targeting the BCR-ABL protein has led to the successful intervention of the disease. Now established as first-line therapy for CML, imatinib is the first selective tyrosine kinase inhibitor of BCR-ABL. Since imatinib only binds to an inactive conformation of the ABL kinase portion, the conformational restrictions contribute to its selectivity. While imatinib has produced clinical remissions in most patients, encounters with subsequent drug resistance are increasing. The culprit is the emergence of mutations in the kinase domain of BCR-ABL that interfere with drug binding. As a second-generation tyrosine kinase inhibitor, dasatinib has been designed to possess less stringent conformational constraints for ABL binding. In practice, dasatinib has demonstrated activity against all imatinib-resistant mutants except the T315I mutant.

Chemical Properties Pale-Yellow Solid

Originator Bristol–Myers Squibb (US)

Uses A new, oral, small-molecule Tyrosine Kinase Inhibitor (TKI) for the treatment of CML. Antineoplastic

Uses Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of ＜1 nM, 0.8 nM and 79 nM, respectively.

Uses Directly targets wild-type and mutant c-Abl kinase domains

Brand name Sprycel (Bristol-Myers Squibb).

General Description Dasatinib is available in 20-, 50-, and 70-mg tablets fororal administration in the treatment of CML and ALL thatare Ph1 positive. Although dasatinib is more potent thanimatinib, bioavailability is much lower with values rangingbetween 14% to 34%. The agent is extensively metabolizedwith as many as 29 metabolites seen as result of oxidationby primarily CYP3A4 and phase II conjugation.The agent may act as an inhibitor of CYP3A4 andCYP2C8. Metabolism does give an active metabolite, but this accounts for only 5% of the total and is not believed tobe important for the overall activity of the agent. Dasatinibis 95% protein bound with a terminal half-life of 3 to5 hours. The majority of the drug and metabolites are eliminatedin the feces. The most common side effects are skinrash, nausea, diarrhea, and fatigue. Serious side effects includemyelosuppression appearing as ne

 

1.Noble Metal Catalysts (Pt.Pd...)

 

2.Organic Phosphine Ligands (Tert-butyl-phosphine.Cyclohexyl-phosphine...)

 

3.OLED intermediates (Fluorene,Carbazole,Boric acid...)

 

4.Customs Synthesis

 

 

 

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