Dasatinib monohydrate

Dasatinib monohydrate Basic information
Product Name:Dasatinib monohydrate
Synonyms:Dasatinib R;BMS-354825 Monohydrate;N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide hydrate;Dasatinib monohydrate N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate;Dasatinib monohydrate, >=99%;dasatinib monohydrate;5-Thiazolecarboxamide, N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-, hydrate (1:1);n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-
CAS:863127-77-9
MF:C22H28ClN7O3S
MW:506.02
EINECS:638-874-6
Product Categories:Inhibitors;API;Molecular Targeted Antineoplastic;SPRYCEL;Anti-cancer&immunity;Pharmaceutical;863127-77-9
Mol File:863127-77-9.mol
Dasatinib monohydrate Structure
Dasatinib monohydrate Chemical Properties
Melting point >223° (dec.)
storage temp. Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility DMSO (Slightly, Sonicated), Methanol (Slightly, Sonicated)
form Solid
color White to Off-White
Stability:Hygroscopic
CAS DataBase Reference863127-77-9(CAS DataBase Reference)
Safety Information
HS Code 29339900
MSDS Information
Dasatinib monohydrate Usage And Synthesis
Usesantineoplastic
UsesDasatinib Monohydrate is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. It is a COVID19-related research product.
DefinitionChEBI: A hydrate that is the monohydrate of dasatinib. It is used for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhyd ous dasatinib (INN).
Brand nameSprycel (Bristol-Myers Squibb).
Biological Activitychronic 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 vitrodasatinib 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 vivomice 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 500.55 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 -
Dasatinib impurity 29 Dasatinib Dasatinib impurity 28 Teniposide MELIBIOSE N-Aminoethylpiperazine Chloroacetic acid 3,4'-DIAMINODIPHENYLMETHANE Dasatinib monohydrate Difluorochloromethane 2-Ethylhexyl ferulate 2-(METHYLSULFONYL)ETHANOL Imatinib Gefitinib Epichlorohydrin Lapatinib Erlotinib Sunitinib

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