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S80002

GDC-0068

源叶(MedMol) 98%
  • 英文名:
  • GDC-0068
  • 别名:
  • (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
  • CAS号:
  • 1001264-89-6
  • 分子式:
  • C24H32ClN5O2
  • 分子量:
  • 458
  • 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) S80002-1mg 98% ¥272.00元 9 0 0 0 EA 加入购物车
源叶(MedMol) S80002-5mg 98% ¥544.00元 5 0 0 0 EA 加入购物车
源叶(MedMol) S80002-10mg 98% ¥748.00元 6 0 0 0 EA 加入购物车
源叶(MedMol) S80002-25mg 98% ¥1360.00元 4 0 0 0 EA 加入购物车
源叶(MedMol) S80002-50mg 98% ¥2244.00元 预计交期:2-3天 0 0 0 EA 加入购物车
源叶(MedMol) S80002-100mg 98% ¥4216.00元 预计交期:2-3天 0 0 0 EA 加入购物车
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参考文献

质检证书(COA)

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  • 提示:详情请下载说明书。
  • 产品描述: Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • 靶点: Akt1:5 nM (IC50);Akt2:18 nM (IC50);Akt3:8 nM (IC50);PKA:3100 nM (IC50)
  • 体内研究:
    Ipatasertib (GDC-0068) is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib (GDC-0068) in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib (GDC-0068) is combined with NSC 241240. The combination of Ipatasertib (GDC-0068) with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone
  • 参考文献:
    1. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27. 2. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.
  • 溶解性: DMSO  :  220  mg/mL  (480.35  mM;  Need  ultrasonic)    H2O  :  3.57  mg/mL  (7.79  mM;  ultrasonic  and  warming  and  heat  to  60°C)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.183 ml 10.917 ml 21.834 ml
    5 mM 0.437 ml 2.183 ml 4.367 ml
    10 mM 0.218 ml 1.092 ml 2.183 ml
    50 mM 0.044 ml 0.218 ml 0.437 ml
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