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S81129

OSI-027

源叶(MedMol) 98%
  • 英文名:
  • OSI-027
  • 别名:
  • (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[1,5-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid
  • CAS号:
  • 936890-98-1
  • 分子式:
  • C21H22N6O3
  • 分子量:
  • 406.45
  • 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) S81129-5mg 98% ¥520.00元 >10 - - - EA 加入购物车
源叶(MedMol) S81129-10mg 98% ¥800.00元 >10 - - - EA 加入购物车
源叶(MedMol) S81129-25mg 98% ¥1600.00元 7 - - - EA 加入购物车
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质检证书(COA)

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  • 提示:详情请下载说明书。
  • 产品描述: OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively
  • 靶点: mTOR:4 nM (IC50);mTORC1:22 nM (IC50);mTORC2:65 nM (IC50);PI3K-γ:0.42 μM (IC50);PI3K-α:1.3 μM (IC50);DNA-PK:1 μM (IC50);Autophagy;DNA-PK; PI3K; mTOR; Autophagy
  • 体内研究:
    Effects on GEO colorectal xenograft growth treated with Rapamycin or OSI-027 for 12 days are consistent with our in vitro experiments. Treatment with Rapamycin (20 mg/kg) inhibits phospho-S6 and phospho-4E-BP1, while Akt phosphorylation is increased by 29%. In contrast, OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors. After 2 hours, decreased 4E-BP1, Akt, and S6 phosphorylation is observed and inhibition of S6 and Akt is sustained for 24 hours. The plasma drug concentration of OSI-027 inversely correlated with these effects on mTORC1 and mTORC2 signaling. The median plasma drug concentration with OSI-027 is 21.3 μM at 2 hours and 14.9 μM at 8 hours. The in vivo efficacy of OSI-027 plus Sunitinib is tested in H292 human lung and Ovcar-5 human ovarian xenograft tumors. H292 tumors, treated with OSI-027 (50 mg/kg) for 21 days have 61% median tumor growth inhibition for the duration of treatment (TGI). Sunitinib (40 mg/kg) for 21 days had 47% median TGI. Combining OSI-027 with Sunitinib, however, has a median TGI of 100% with 59% maximal tumor regression, a statistically significant improvement over either agent alone. Ovcar-5 xenograft tumors treated with OSI-027 or Sunitinib have a 55% and 68% median TGI, respectively. OSI-027 administered with Sunitinib has a significantly better median TGI of 100% with 38% maximal tumor regression. In the Rapamycin (RAPA) group, three rats exhibit symptoms typical of LTx-aGVHD and die 27 to 35 days after liver transplantation (LT); the remaining five r
  • 参考文献:
    1. Falcon BL, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. 2. Mateo J, et al. A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies. Br J Cancer. 2016;114(8):889-896. 3. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56. 4. Zhi X, et al. OSI-027 modulates acute graft-versus-host disease after liver transplantation in a rat model. Liver Transpl. 2017 Sep;23(9):1186-1198.
  • 溶解性: DMSO  :  125  mg/mL  (307.55  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.46 ml 12.302 ml 24.603 ml
    5 mM 0.492 ml 2.46 ml 4.921 ml
    10 mM 0.246 ml 1.23 ml 2.46 ml
    50 mM 0.049 ml 0.246 ml 0.492 ml
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