S80048
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- 公司名稱 上海源葉生物科技有限公司
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- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時間 2025/5/15 19:34:15
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- 產(chǎn)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
- 靶點： 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)
- 體內(nèi)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
- 參考文獻(xiàn)：
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.
- 溶解度： DMSO : 25 mg/mL (78.03 mM; Need ultrasonic)H2O : < 0.1 mg l (ultrasonic;warming;heat to 80°c) (insoluble)="">
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 3.121 ml 15.606 ml 31.212 ml 5 mM 0.624 ml 3.121 ml 6.242 ml 10 mM 0.312 ml 1.561 ml 3.121 ml 50 mM 0.062 ml 0.312 ml 0.624 ml
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