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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 | | EINECS: | | | Product Categories: | Inhibitor;Apis;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 827318-97-8.mol |  |
| | 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 |
| | 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 |
| | Danusertib Preparation Products And Raw materials |
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