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S80048

MK-4827 (Niraparib)

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  • 英文名:
  • MK-4827 (Niraparib)
  • 别名:
  • 2-[4-((3S)-3-哌啶基)苯基]-2H-吲唑-7-甲酰胺;(S)-2-(4-(哌啶-3-基)苯基)-2H-吲唑-7-羧酰胺;MK4827; 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;
  • CAS号:
  • 1038915-60-4
  • 分子式:
  • C19H20N4O
  • 分子量:
  • 320.39
  • 核磁/质谱:
货号产品规格市场价(RMB)您的折扣价(RMB)库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
S80048-1mg 99% ¥320.00元 ¥217.60元 >10 0 0 0 EA 加入购物车
S80048-2mg 99% ¥450.00元 ¥306.00元 >10 0 0 0 EA 加入购物车
S80048-5mg 99% ¥600.00元 ¥408.00元 >10 0 0 0 EA 加入购物车
S80048-10mg 99% ¥890.00元 ¥605.20元 >10 0 0 0 EA 加入购物车
S80048-25mg 99% ¥1200.00元 ¥816.00元 >10 0 0 0 EA 加入购物车
S80048-50mg 99% ¥1700.00元 ¥1156.00元 >10 0 0 0 EA 加入购物车
S80048-100mg 99% ¥3200.00元 ¥2176.00元 >10 0 0 0 EA 加入购物车
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  • 提示:详情请下载说明书。
  • 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)
  • 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:
    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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