| 中文名称: | 甲苯磺酸尼拉帕尼一水合物 | ||||
|---|---|---|---|---|---|
| 英文名称: | Niraparib Tosylate Monohydrate | ||||
| 别名: | Niraparib (tosylate hydrate) | ||||
| CAS No: | 1613220-15-7 | 分子式: | C26H30N4O5S | 分子量: | 510.61 |
| CAS No: | 1613220-15-7 | ||||
| 分子式: | C26H30N4O5S | ||||
| 分子量: | 510.61 | ||||
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
Niraparib (MK-4827) tosylate hydrate 是高效的，具有生物口服利用度的 PARP1 和 PARP2 抑制剂，IC50 分别为 3.8 nM 和 2.1 nM。Niraparib tosylate hydrate 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。
储备液保存：
-80°C, 6 months
-20°C, 1 month
(sealed storage, away from moisture)
-20°C, 1 month
(sealed storage, away from moisture)
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)
PARP-1: 3.8 nM (IC50)
V-PARP: 330 nM (IC50)
TANK-1：570 nM (IC50)
PARP-3：1300 nM (IC50)
体外研究：
Niraparib (MK-4827) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. Niraparib tosylate hydrate inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. Niraparib tosylate hydrate displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay.
Niraparib tosylate hydrate inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.
Niraparib tosylate hydrate inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.
体内研究：
Niraparib (MK-4827) tosylate hydrate is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
Niraparib (MK-4827) tosylate hydrate is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
Niraparib (MK-4827) tosylate hydrate 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) tosylate hydrate 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.
Niraparib (MK-4827) tosylate hydrate is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
Niraparib (MK-4827) tosylate hydrate 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) tosylate hydrate 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.
保存条件：
-20℃
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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