包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cell lines | human MCF-7 and SKBr-3 breast cancer cells |
Preparation method | The solubility of this compound in DMSO is >16.35mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 5-50 μM, 48 and 72h |
Applications | In human MCF-7 and SKBr-3 breast cancer cells, AZD2461 was cytotoxic and reduced numbers of viable cells in a concentration- and time-dependent manner. PARP-1 inhibition by AZD2461 (10 μM for 48h) increased proportions of MCF-7 cells in the G2 phase and reduced cells in S-phase. |
Animal models | mice with KB1P tumors |
Dosage form | 100 mg/kg p.o., 28 consecutive days or 100 consecutive days |
Application | In mice with KB1P tumors, AZD2461 completely inhibited the PARP activity for several hours and the amount of PARP returned to baseline levels 24 hours after treatment. AZD2461 had lower affinity for Pgp than did olaparib. Mice treated with AZD2461 for 28 consecutive days showed increased survival. When treatment with AZD2461 for 100 consecutive days, 8 of 9 mice engrafted with fragments from 3 individual KB1P tumors did not develop refractory tumors within 300 days after treatment start. Long-term AZD2461 treatment was well tolerated and doubled the median relapse-free survival from 64 to 132 days. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | AZD2461 is a novel PARP inhibitor with IC50 value of 5nM [1]. |