Danusertib (PHA-739358)
Danusertib (PHA-739358)
CAS: 827318-97-8
Molecular Formula: C26H30N6O3
Danusertib (PHA-739358) - Names and Identifiers
Danusertib (PHA-739358) - Physico-chemical Properties
| Molecular Formula | C26H30N6O3 |
| Molar Mass | 474.55 |
| Density | 1.322 |
| Melting Point | >145°C (dec.) |
| Boling Point | 664.1±55.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Pale Beige |
| pKa | 13.70±0.20(Predicted) |
| Storage Condition | Refrigerator |
| Use | Danusertib (PHA-739358) is an Aurora kinase inhibitor. When it acts on Aurora A/B/C, its IC50 is 13 nM/79 nM/61 nM. It acts moderately and effectively on Abl, TrkA, c-RET and FGFR1, and has slightly weaker effects on Lck, VEGFR2/3, c-Kit, CDK2, etc. |
| In vitro study | Danusertib also inhibits the activity of other kinases, such as FGFR1, Abl, Ret, and Trka, with IC50 of 47, 25, 31, and 31 nM, respectively. When wild-type MEFs and p53-deficient MEFs were treated with Danusertib, wild-type cells were inhibited in mitosis (4N) and arrested for 48 h, however, p53 deficient cells are not inhibited when DNA is 4N, and continue mitosis, DNA becomes> 8N. Danusertib treatment led to an increase in p53 protein levels and also to an increase in p21 protein, which p53 regulates at the transcriptional level. |
| In vivo study | In an in vivo study, 25 mg/kg of Danusertib injected intravenously into HL-60 transplanted mice inhibited tumor growth by 75%. In Vivo, Danusertib leads to the regulation of biological markers, accompanied by appropriate inhibition of tumor growth and the expected inhibition of aurora kinase activity mechanisms. |
Danusertib (PHA-739358) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.107 ml | 10.536 ml | 21.073 ml |
| 5 mM | 0.421 ml | 2.107 ml | 4.215 ml |
| 10 mM | 0.211 ml | 1.054 ml | 2.107 ml |
| 5 mM | 0.042 ml | 0.211 ml | 0.421 ml |
Last Update：2024-01-02 23:10:35
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View History
Danusertib (PHA-739358)
2-(氮杂环丁烷-3-基氧基)乙酸
4,6-二氯-2-甲基-5-(1-乙酰基-2-咪唑啉-2)-氨基嘧啶
Tofacitinib Impurity N (Citrate)
5-2-乙酰基吡嗪-2-甲酰胺
(4R,6R)-1,3-二氧杂环己烷-4-乙酸 6-[2-[2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4-[(苯氨基)羰基]-1H-吡咯-1-基]乙基]-2,2-二甲基-1,1-二甲基乙酯
Lithium tri-tert-butoxyaluminum hydride
(S)-β-(2-methoxyphenyl)-β-aminopropionic acid
(4-Ethoxy-3-methoxyphenyl)methanol
N'-METHYL-N'-[2-(METHYLSULFANYL)-4-QUINAZOLINYL]-2-THIOPHENECARBOHYDRAZIDE
2-(氮杂环丁烷-3-基氧基)乙酸
4,6-二氯-2-甲基-5-(1-乙酰基-2-咪唑啉-2)-氨基嘧啶
Tofacitinib Impurity N (Citrate)
5-2-乙酰基吡嗪-2-甲酰胺
(4R,6R)-1,3-二氧杂环己烷-4-乙酸 6-[2-[2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4-[(苯氨基)羰基]-1H-吡咯-1-基]乙基]-2,2-二甲基-1,1-二甲基乙酯
Lithium tri-tert-butoxyaluminum hydride
(S)-β-(2-methoxyphenyl)-β-aminopropionic acid
(4-Ethoxy-3-methoxyphenyl)methanol
N'-METHYL-N'-[2-(METHYLSULFANYL)-4-QUINAZOLINYL]-2-THIOPHENECARBOHYDRAZIDE