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S82582

ETP-46321

源叶(MedMol) 98%
  • 英文名:
  • ETP-46321
  • 别名:
  • 5-(2-((4-sulfonylmethylpiperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine; ETP-46321; ETP46321; ETP-46321; ETP 46321
  • CAS号:
  • 1252594-99-2
  • 分子式:
  • C20H27N9O3S
  • 分子量:
  • 473.5519
  • 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) S82582-5mg 98% ¥1020.00元 5 - - - EA 加入购物车
源叶(MedMol) S82582-10mg 98% ¥1700.00元 5 - - - EA 加入购物车
源叶(MedMol) S82582-25mg 98% ¥3400.00元 5 - - - EA 加入购物车
源叶(MedMol) S82582-100mg 98% ¥10200.00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: ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).
  • 靶点: PI3K
  • 体外研究:
    ETP-4632 has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K, and H1047R), being equipotent against these mutants when compared to the wild type protein (Kiapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorylation of AKT in the U2OS cell line (IC50: 8.3 nM).
  • 体内研究:
    ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition
  • 动物实验: BALB/C mice are treated daily with ETP-46321 (50 mg/kg, p.o.) for three weeks. Tumor volumes of four mice in each treatment group are measured and compared to the starting volume at the beginning of the treatment.
  • 参考文献:
    1. Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J. Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.112 ml 10.559 ml 21.117 ml
    5 mM 0.422 ml 2.112 ml 4.223 ml
    10 mM 0.211 ml 1.056 ml 2.112 ml
    50 mM 0.042 ml 0.211 ml 0.422 ml
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