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S80220

VS-5584 (SB2343)

源叶(MedMol) 99%
  • 英文名:
  • VS-5584 (SB2343)
  • 别名:
  • 2-Pyrimidinamine, 5-[8-methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-
  • CAS号:
  • 1246560-33-7
  • 分子式:
  • C17H22N8O
  • 分子量:
  • 354.41
  • 核磁/质谱:
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源叶(MedMol) S80220-5mg 99% ¥340.00元 7 - - - EA 加入购物车
源叶(MedMol) S80220-10mg 99% ¥489.60元 7 - - - EA 加入购物车
源叶(MedMol) S80220-50mg 99% ¥2250.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
  • 靶点: PI3Kα:16 nM (IC50);PI3Kγ:25 nM (IC50);PI3Kδ:42 nM (IC50);PI3Kβ:68 nM (IC50);Vps34:7470 nM (IC50);mTOR:37 nM (IC50);mTORC1;mTORC2;DNA-PK:1270 nM (IC50);PI3K;mTOR
  • 体内研究:
    Nude mice bearing MDA-MB-231 human breast cancer tumors are treated for 5 days with once daily oral VS-5584 (25 mg/kg). Oral treatment of tumor bearing mice with VS-5584 reduces cancer atem cells analyzed from extracted tumors. Mice are implanted with tumor fragments from a docetaxel-resistant patient-derived triple negative breast cancer. Mice are treated with VS-5584 (20 mg/kg, po, qd) or Docetaxel (20 mg/kg, i.v.). Oral VS-5584 induces tumor regression in a Docetaxel-resistant patient-derived breast cancer model. A single oral dose of VS-5584 is rapidly absorbed with a tmax of 0.9 hours and an elimination half-life of 10 hours. To determine the pharmacokinetic and pharmacodynamic relationship in tumors, PC3-tumor–bearing mice are treated with a single dose of VS-5584 and plasma and tumors are harvested after 6 hours and analyzed for concentrations of VS-5584 and effects on target efficacy biomarkers. Plasma levels of VS-5584 increase dose-dependently. For evaluation of efficacy in a Rapamycin-sensitive PC3 engraftment model, tumor-bearing mice are treated with VS-5584 for 28 days in comparison with the rapalog Everolimus. VS-5584 is well tolerated at both doses tested (11 and 25 mg/kg) with minimal weight loss (mean 4.7% on day 27). Treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively
  • 参考文献:
    1. Hart S, et al. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther, 2013, 12(2), 151-161.
  • 溶解性: DMSO  :  33.33  mg/mL  (94.04  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.822 ml 14.108 ml 28.216 ml
    5 mM 0.564 ml 2.822 ml 5.643 ml
    10 mM 0.282 ml 1.411 ml 2.822 ml
    50 mM 0.056 ml 0.282 ml 0.564 ml
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