| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S80048-1mg买3赠1 |
99.80% | ￥216.00 |
>10 | - | - | - | - |
|
S80048-2mg买3赠1 |
99.80% | ￥306.00 |
>10 | - | - | - | - |
|
S80048-5mg买3赠1 |
99.80% | ￥408.00 |
>10 | - | - | - | - |
|
S80048-10mg买3赠1 |
99.80% | ￥605.00 |
>10 | - | - | - | - |
|
S80048-25mg买3赠1 |
99.80% | ￥816.00 |
>10 | - | - | - | - |
|
S80048-50mg买3赠1 |
99.80% | ￥1150.00 |
>10 | - | - | - | - |
|
S80048-100mg买3赠1 |
99.80% | ￥2170.00 |
>10 | - | - | - | - |
|
| 产品描述： | Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | PARP-2：2.1 nM (IC50)；PARP-1：3.8 nM (IC50)；V-PARP：330 nM (IC50)；TANK-1：570 nM (IC50)；PARP-3：1300 nM (IC50);Apoptosis;PARP | ||||||||||||||||||||
| 体内研究： | Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily | ||||||||||||||||||||
| 参考文献： | 1. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85. 2. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86. 3. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20. 4. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164. | ||||||||||||||||||||
| 溶解性： | DMSO : 25 mg/mL (78.03 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble) | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京