Danusertib

Danusertib Basic information
Product Name:Danusertib
Synonyms:PHA-739358;(R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide,PHA739358;Benzamide, 4-(4-methyl-1-piperazinyl)-N-(1,4,5,6-tetrahydro-5-((2R)- methoxyphenylacetyl)pyrrolo(3,4-C)pyrazol-3-yl)-;Unii-m3X659D0fy;Danusertib(PHA-739358);danusertib;N-[5-((2R)-2-Methoxy-2-phenylethanoyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide;PHA-739358(Danusertib)
CAS:827318-97-8
MF:C26H30N6O3
MW:474.55
EINECS:
Product Categories:Inhibitor;Apis;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:827318-97-8.mol
Danusertib Structure
Danusertib Chemical Properties
Melting point >145°C (dec.)
Boiling point 664.1±55.0 °C(Predicted)
density 1.322
storage temp. Refrigerator
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
pka13.70±0.20(Predicted)
color Pale Beige
Safety Information
MSDS Information
Danusertib Usage And Synthesis
UsesDanusertib is an Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia.
UsesAn Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia. It is a COVID19-related research product.
DefinitionChEBI: N-[5-[(2R)-2-methoxy-1-oxo-2-phenylethyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methyl-1-piperazinyl)benzamide is a member of piperazines.
Biological Activitydanusertib (previously known as pha-739358), a 3-aminopyrazole derivative identified during the development of the pyrrolopyrazole sub-series, is a potent small-molecule inhibitor of aurora kinases family members with a dominant inhibition for aurora b kinase (abk). this pan-aurora kinases inhibitor is also able to inhibit several tyrosine kinases, including t315i mutant, ret, trk-a and fibroblast growth factor receptor-1 (fgfr-1), which are involved in multiple malignancies, such as chronic myelogenous leukemia (cml), acute lymphoblastic leukemia (all), thyroid prostate and breast carcinoma. thus, in many previous studies, danusertib exhibits remarkable antitumor activity in a number of different xengorafts, spontaneous, and transgenic animal tumor models with a favorable pharmacokinetic and safety profile.carpinelli p, ceruti r, giorgini ml, cappella p, gianellini l, croci v, degrassi a, texido g, rocchetti m, vianello p, rusconi l, storici p, zugnoni p, arrigoni c, soncini c, alli c, patton v, marsiglio a, ballinari d, pesenti e, fancelli d, moll j. pha-739358, a potent inhibitor of aurora kinases with a selecyive target inhibiton profile relevant to cancer. mol cancer ther 2007; 6(12 pt 1): 3158-3168
targetAurora A/B/C
Danusertib Preparation Products And Raw materials
Tadalafil Dasatinib PHA-793887 Pralmorelin 4'-Methoxyacetophenone N-ACETYL-L-TYROSINE ETHYL ESTER 4-Methoxybenzylchloride Methoxy 4-Methoxyphenylacetone 2-Methoxyethanol Anisole (Trifluoromethoxy)benzene p-Anisidine p-Anisaldehyde Danusertib Pyrrolidine

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