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Dasatinib

Leukemia drug Chemical properties Uses
Dasatinib
Dasatinib structure
CAS No.
302962-49-8
Chemical Name:
Dasatinib
Synonyms
CS-1968;Dasatinib;BMS-354825;NCGC00181129;25MG/100MG/1G;Dasatinib, 95+%;sprycel Dasatinib;DASATINIB HCL 99%;Dasatinib Tablets;BMS-354825; SPRYCEL
CBNumber:
CB4506696
Molecular Formula:
C22H26ClN7O2S
Formula Weight:
488.01
MOL File:
302962-49-8.mol

Dasatinib Properties

Melting point:
275-286°C
Density 
1.408±0.06 g/cm3(Predicted)
storage temp. 
-20°C Freezer
pka
10.94±0.70(Predicted)
form 
White powder.
CAS DataBase Reference
302962-49-8(CAS DataBase Reference)
FDA UNII
RBZ1571X5H
NCI Dictionary of Cancer Terms
BMS-354825; dasatinib
SAFETY
  • Risk and Safety Statements
HS Code  29341000

Dasatinib price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 11498 Dasatinib ≥98% 302962-49-8 10mg $25 2021-03-22 Buy
Cayman Chemical 11498 Dasatinib ≥98% 302962-49-8 50mg $35 2021-03-22 Buy
Cayman Chemical 11498 Dasatinib ≥98% 302962-49-8 100mg $63 2021-03-22 Buy
Cayman Chemical 11498 Dasatinib ≥98% 302962-49-8 250mg $125 2021-03-22 Buy

Dasatinib Chemical Properties,Uses,Production

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

Dasatinib, developed and marketed by Bristol Myers, is the first approved oral tyrosine kinase inhibitor which binds to multiple conformations of ABL kinase for the treatment of two leukemia indications: chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Dasatinib is a highly potent, ATPcompetitive ATPcompetitive kinase inhibitor which, at nanomolar concentrations, inhibits BCR-ABL, SRC family, c-KIT, EPHA2 and PDGFR-B.

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 neutropenia andthrombocytopenia, bleeding of the brain and GI tract, andfluid retention.

Chemical Synthesis

A concise and efficient route was developed for the synthesis of dasatinib. Reaction of 2-chlorothioa-zole (18) with n-butyllithium at low temperature followed by addition of 2-chloro-6-methylphenyl isocyanate (19) gave anilide 20 in 86% yield. The amide 20 was protected as corresponding 4-methoxy benzyl (PMB) anilide 22 in 95% yield which was subsequently reacted with 4- amino-6-chloro-2-methylpyrimidine (23) in the presence of sodium hydride in hot THF to give compound 24 in 83% yield. The PMB protecting group was then removed with triflic acid to give compound 25 in 99% yield. Compound 25 was reacted with 1-(2-hydroxyethyl)piperazine (26) in refluxing dioxane to give dasatinib (III) in 91% yield.

Dasatinib Preparation Products And Raw materials

Raw materials

Preparation Products


Dasatinib Suppliers

Global( 377)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Biocare Pharmaceutical Ltd
+86-23-63023096
contact@boeingpharm.com CHINA 2 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20010 60
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22608 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8875 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26699 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
Hebei Chisure Biotechnology Co.LTD
13292891350 +86 13292890173
luna@speedgainpharma.com CHINA 1010 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29991 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58

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View Lastest Price from Dasatinib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-06-17 Dasatinib
302962-49-8
US $63.50-2063.50 / KG 10g 99% 100KG Baoji Guokang Healthchem co.,ltd
2018-07-30 Dasatinib
302962-49-8
US $10.00 / KG 10ASSAYS 99% 500kg/month Hebei Chisure Biotechnology Co.LTD
2021-05-13 dasatinib
302962-49-8
US $275.00 / KG 1KG 99% 9000kg/per week Hebei Lingding Biological Technology Co., Ltd

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