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S80013

AZD8055

源叶(MedMol) 98%
  • 英文名:
  • (5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
  • 别名:
  • 5-[2,4-双[(3S)-3-甲基-4-吗啉]吡啶并[2,3-d]嘧啶-7-基]-2-甲氧基苯甲醇;[5-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol
  • CAS号:
  • 1009298-09-2
  • 分子式:
  • C25H31N5O4
  • 分子量:
  • 465.56
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80013-5mg 98% ¥183.60元 >10 - - - EA 加入购物车
源叶(MedMol) S80013-10mg 98% ¥204.00元 >10 - - - EA 加入购物车
源叶(MedMol) S80013-25mg 98% ¥476.00元 >10 - - - EA 加入购物车
源叶(MedMol) S80013-50mg 98% ¥612.00元 >10 - - - EA 加入购物车
源叶(MedMol) S80013-100mg 98% ¥1070.00元 >10 - - - EA 加入购物车
源叶(MedMol) S80013-200mg 98% ¥1632.00元 8 - - - EA 加入购物车
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参考文献

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  • 提示:详情请下载说明书。
  • 产品描述: AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2
  • 靶点: mTOR:0.8 nM (IC50);mTORC1;mTORC2;Autophagy;Apoptosis;mTOR;Autophagy
  • 体内研究:
    In mice bearing U87-MG (PTEN null) glioblastoma xenografts, oral treatment with AZD-8055 (AZD8055) results in a dose-dependent tumor growth inhibition of 33%, 48%, and 77% with 2.5, 5, and 10 mg/kg/d twice daily, respectively. A similar dose dependency is observed in nude mice bearing A549 xenografts: tumor growth inhibition is 44%, 55%, and 93% after 2.5, 5, and 10 mg/kg/d twice daily, respectively. AZD8055 also results in significant inhibition of tumor growth and/or regression in breast, lung, colon, prostate, and uterine xenograft models when administered either twice daily at 10 mg/kg or daily at a dose of 20 mg/kg. AZD8055 markedly decreases the phosphorylation levels of mTOR and its substrates and the activation of microglia in vivo, and promotes the microglial polarization from M1 phenotype to M2 phenotype. In addition, administration of AZD8055 following subarachnoid hemorrhage (SAH) significantly ameliorates EBI, including neuronal apoptosis, neuronal necrosis, brain edema and blood-brain barrier permeability
  • 参考文献:
    1. Chresta CM, et al. AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res, 2010, 70(1), 288-298.2. You W, et al. Inhibition of mammalian target of rapamycin attenuates early brain injury through modulating microglial polarization after experimental subarachnoid hemorrhage in rats. J Neurol Sci. 2016 Aug 15;367:224-31. 3. Kawata T, et al. Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. Cancer Sci. 2017 Oct 27.
  • 溶解性: DMSO  :  33.33  mg/mL  (71.59  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.148 ml 10.74 ml 21.48 ml
    5 mM 0.43 ml 2.148 ml 4.296 ml
    10 mM 0.215 ml 1.074 ml 2.148 ml
    50 mM 0.043 ml 0.215 ml 0.43 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)


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