|4-[4-氟-3-[(4-甲氧基哌啶-1-基)羰基]苄基]酞嗪-1(2H)-酮|CsnPharm

CAS No.: 1174043-16-3

AZD-2461 Catalog No. CSN16496

Synonyms: AZD2461

AZD2461 is a PARP inhibitor, which has the potential to avoid the olaparib resistence mediated by Pgp.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The inhibition of poly (ADP-ribose) polymerases (PARP) has been used as a therapeutic strategy for homologous recombination–deficient tumors. AZD2461 is a potent inhibitor of both PARP1 and PARP2 with IC50 values of 5 nM and 2 nM, respectively. In human A549 cells, 500 nM AZD2461 inhibited poly (ADP-ribose) polymers formation following the treatment with 10 mM hydrogen peroxide. AZD2461 at 500 nM also augmented the anti-proliferative effect of the DNA-damaging alkylating agent MMS in HeLa cells. In colorectal cancer cell line HCT-15, the activity of AZD2461 alone or in combination with the P-gp inhibitor verapamil showed the IC50 values of 6.4 and 5.7 μM, respectively^[4]. In vivo, a single p.o. administration of 100 mg/kg AZD2461 completely inhibited the PARP activity for a couple of hours and then returned to baseline level 24 hours after the treatment. Compared to olaparib-treated animals, consecutive oral administration of AZD2461 (100 mg/kg) for 28 days increased the survival rate in mice with KB1P tumors, but all mice eventually developed refractory tumors. When AZD2461 treatment was extended to 100 consecutive days, 8 out of 9 mice showed no relapsing tumors within 300 days after the treatment began^[5].
作用机制AZD2461 is an orally available compound with lower affinity to P-glycoprotein. It selectively binds to PARP, inhibiting PARP-mediated DNA repair^[4].
动物研究
剂量
Rat: 10 mg/kg, 20 mg/kg^[2] (p.o.) Mice: 100 mg/kg^[3] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Rat: 10 mg/kg, 20 mg/kg^[2] (p.o.) Mice: 100 mg/kg^[3] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01247168	Refractory Solid Tumors ... more >> Cancer Tumor Collapse <<	Phase 1	Completed	-	United States, Tennessee ... more >> Research Site Nashville, Tennessee, United States Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5289 mL
- 12.6446 mL
- 25.2891 mL
- 5 mM
- 0.5058 mL
- 2.5289 mL
- 5.0578 mL
- 10 mM
- 0.2529 mL
- 1.2645 mL
- 2.5289 mL

技术信息

CAS号

1174043-16-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H22FN3O3

运输

蓝冰

分子量

395.43

别名

AZD2461

溶解度

DMSO	79.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	30.0 mg/mL (75.9 mM)

动物实验配方

2% DMSO+40% PEG 300+2% Tween 80+water

5 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

AZD-2461 Catalog No. CSN16496

靶点选择性

请登录您的专属账户

确认信息