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| 化学名: | ダヌセルチブ | | 英語化学名: | Danusertib | | 别名: | 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番号: | 827318-97-8 | | 分子式: | C26H30N6O3 | | 分子量: | 474.55 | | EINECS: | | | カテゴリ情報: | Inhibitor;Apis;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 827318-97-8.mol |  |
| 融点 | >145°C (dec.) | | 沸点 | 664.1±55.0 °C(Predicted) | | 比重(密度) | 1.322 | | 貯蔵温度 | Refrigerator | | 溶解性 | DMSO (Slightly), Methanol (Slightly) | | 外見 | Solid | | 酸解離定数(Pka) | 13.70±0.20(Predicted) | | 色 | Pale Beige |
| | ダヌセルチブ Usage And Synthesis |
| 使用 | An Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia. It is a COVID19-related research product. | | 使用 | Danusertib is an Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia. | | 定義 | 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. | | 生物活性 | 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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