AZD2461CAS号： 1174043-16-3分子式： C22H22FN3O3分子量： 395.43描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
AZD2461是一种新型PARP抑制剂，作用于Pgp比Olaparib亲和力低。AZD2461作用于Pgp比Olaparib亲和力低。 |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
AZD-2461
|
| 可溶性/溶解性 |
Ethanol ：39.5 mg/mL (100 mM)
DMSO ：39.5 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 |
PARP
|
| In vitro(体外研究) |
AZD2461 has lower affinity for Pgp than does Olaparib.
|
| In vivo(体内研究) |
AZD2461 has an 80-fold increased Mdr1b expression on Olaparib-resistant KB1P tumor T6-28, without inhibition of Pgp. AZD2461 induces loss of 53BP1 expression in mice with KB1P tumors with short-term treatment. Long-term AZD2461 treatment is well tolerated and doubled the median relapse-free survival.
|
| 参考文献 | |
| 参考文献 |
Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors.
Jaspers JE,et al. Cancer Discov. 2013 Jan;3(1):68-81. PMID: 23103855 |
分子结构图
