863127-77-9 Usage
Description
Dasatinib monohydrate is a synthetic small molecule inhibitor of SRC-family protein-tyrosine kinases, which is an orally bioavailable compound. It has been identified as a COVID-19 related research product, indicating its potential role in the study and treatment of the virus.
Uses
Used in Antineoplastic Applications:
Dasatinib monohydrate is used as an antineoplastic agent for its ability to inhibit the activity of SRC-family protein-tyrosine kinases, which play a crucial role in the growth and proliferation of cancer cells. By targeting these kinases, Dasatinib monohydrate can help control tumor growth and potentially lead to the regression of cancerous masses.
Used in COVID-19 Research:
Dasatinib monohydrate is used as a research product in the context of COVID-19, where it may contribute to the understanding of the virus's mechanisms and the development of potential therapeutic interventions. Its role in this research could be multifaceted, including the exploration of its effects on viral replication, immune response modulation, or other pathways relevant to COVID-19 infection and treatment.
Biological Activity
chronic myeloid leukemia (cml) is a disease characterized by the presence of the philadelphia (ph+) chromosome and its oncogenic product, bcr-abl, that is present in >90% of the patients. dasatinib (bms-354825) is a novel, potent, and multitargeted kinase inhibitor that targets abl, src, kit, pdgfr, and other tyrosine kinases.
in vitro
dasatinib is a potent atp-competitive inhibitor in biochemical assays with broad-spectrum antiproliferative activities against hematological and solid tumor cell lines. dasatinib was more potent than imatinib at inhibiting nonmutated bcr-abl kinase activity. in addition, the kinase activity of 14 out of 15 different clinically relevant, imatinib-resistant bcr-abl isoforms was successfully inhibited [1].
in vivo
mice were dosed with dasatinib or vehicle alone by gavage for 2 weeks, beginning 3 days after injection of ba/f3 cells. all vehicle-treated mice developed progressive disease. in contrast, dasatinib–treated mice harboring nonmutant bcr-abl or the clinically common imatinib-resistant mutation m351t appeared healthy with no evidence of weight loss, lethargy, or ruffled fur and showed more than one log lower levels of bioluminescent activity after 2 weeks of therapy [2].
IC 50
0.55 and 3.0 nm for src and bcr-abl tyrosine kinases, respectively
references
[1] shah np, tran c, lee fy, chen p, norris d, sawyers cl. overriding imatinib resistance with a novel abl kinase inhibitor. science. 2004 jul 16;305(5682):399-401.[2] monika conchon, carla maria boquimpani de moura freitas, maria aparecida do carmo rego, and josé wilson ramos braga junior. dasatinib -
Check Digit Verification of cas no
The CAS Registry Mumber 863127-77-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,3,1,2 and 7 respectively; the second part has 2 digits, 7 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 863127-77:
(8*8)+(7*6)+(6*3)+(5*1)+(4*2)+(3*7)+(2*7)+(1*7)=179
179 % 10 = 9
So 863127-77-9 is a valid CAS Registry Number.
InChI:InChI=1/C22H27N7O2S2.H2O/c1-14-4-3-5-16(32)20(14)27-21(31)17-13-23-22(33-17)26-18-12-19(25-15(2)24-18)29-8-6-28(7-9-29)10-11-30;/h3-5,12-13,30,32H,6-11H2,1-2H3,(H,27,31)(H,23,24,25,26);1H2
863127-77-9Relevant articles and documents
Preparation method for dasatinib monohydrate
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Paragraph 0041; 0072-0073, (2020/07/13)
The invention provides a preparation method for a dasatinib monohydrate. The dasatinib monohydrate is obtained by a reaction of dasatinib in an ethanol aqueous solution. According to a technical scheme of the invention, the high-quality dasatinib monohydrate can be obtained; tedious separation and purification steps are avoided; operation is simple; the waste of raw materials is also avoided; theproduction cost is reduced; and the preparation method is more applicable to industrial production.
A convenient new and efficient commercial synthetic route for dasatinib (Sprycel)
Suresh, Garbapu,Nadh, Ratnakaram Venkata,Srinivasu, Navuluri,Yennity, Durgaprasad
, p. 1610 - 1621 (2017/09/08)
A new and efficient synthetic route for dual-Src/Abl kinase inhibitor dasatinib (Sprycel), an anticancer drug, is described. This commercially viable process yields dasatinib monohydrate free of potential impurities with consistent yield of 68% in route A and 61% in route B with HPLC purity >99.80% over four stages.
ORAL ADMINISTRATION OF N-(2-CHLORO-6-METHYLPHENYL)-2-[[6-[4-(2-HYDROXYETHYL)-1-PIPERAZINYL]-2-METHYL-4-PYRIMIDINYL]AMINO]-1,3-THIAZOLE-5-CARBOXAMIDE AND SALTS THEREOF
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Page/Page column 57-58, (2010/11/26)
Disclosed are a method of treating cancer and/or other proliferative diseases comprising orally administering N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof, and pharmaceutical compositions comprising N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof. Also disclosed are N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide salts, as well as crystalline forms thereof.