| Identification | Back Directory | [Name]
KU59403 | [CAS]
845932-30-1 | [Synonyms]
KU59403
3-(4-methylpiperazin-1-yl)-N-[6-(6-morpholin-4-yl-4-oxopyran-2-yl)thianthren-2-yl]propanamide
3-(4-methylpiperazin-1-yl)-N-(6-(6-morpholino-4-oxo-4H-pyran-2-yl)thianthren-2-yl)propanamide
1-Piperazinepropanamide, 4-methyl-N-[6-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-2-thianthrenyl]- | [Molecular Formula]
C29H32N4O4S2 | [MOL File]
845932-30-1.mol | [Molecular Weight]
564.72 |
| Chemical Properties | Back Directory | [Boiling point ]
814.3±65.0 °C(Predicted) | [density ]
1.368±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
13.73±0.20(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
KU 59403 is an Ataxia telangiectasia mutated inhibitor (ATM inhibitor) in models of human cancer. | [in vivo]
KU59403 with a single daily dose of 12.5 mg/kg causes a significant sensitization[1].
Increasing the dose of KU59403 to 25 mg/kg given twice daily results in the greatest chemo-sensitisation with a 3-fold increase in BMY-40481-induced tumour growth delay in both SW620 and HCT116-N7 xenografts, in the absence of a significantly increased toxicity[1].
| Animal Model: | CD-1 nude mice implanted with SW620 or HCT116-N7 human cancer cell lines at 1×107 cells per animal s.c. (n=5 per group)[1]. | | Dosage: | 6, 12.5 and 25 mg/kg. | | Administration: | I.P. twice daily (0 and 4 hours) and 12.5 mg/kg once daily. | | Result: | Treatment with BMY-40481 alone causes a modest tumour growth delay of 4 days (time to RTV4=10.5 days). This delay is extended to 8.5 days when given with KU 59403 at 12.5 mg/kg i.p. twice daily for 5 days and 11.5 days (time to RTV4=18 days) when given with KU 59403 at 25 mg/kg i.p. twice daily for 5 days. |
| [storage]
Store at -20°C |
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