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Danusertib

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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
Product Categories:
  • Inhibitor
  • Apis
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
827318-97-8.mol
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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
pka
13.70±0.20(Predicted)
color 
Pale Beige
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Danusertib Usage And Synthesis

Uses

An Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia. It is a COVID19-related research product.

Uses

Danusertib is an Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia.

Definition

ChEBI: 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 Activity

danusertib (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

target

Aurora A/B/C

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