生物活性 靶点 体外研究 体内研究 2-氯-1-(1H-吲哚-3-基)-乙酮 试剂级价格
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2-氯-1-(1H-吲哚-3-基)-乙酮

2-氯-1-(1H-吲哚-3-基)-乙酮,28755-03-5,结构式
2-氯-1-(1H-吲哚-3-基)-乙酮
  • CAS号:28755-03-5
  • 英文名:Ethanone, 2-chloro-1-(3-indolyl)-
  • 中文名:2-氯-1-(1H-吲哚-3-基)-乙酮
  • CBNumber:CB41247653
  • 分子式:C10H8ClNO
  • 分子量:193.63
  • MOL File:28755-03-5.mol
2-氯-1-(1H-吲哚-3-基)-乙酮化学性质
  • 熔点 :212-214 °C(Solv: ethyl ether (60-29-7))
  • 沸点 :379.1±17.0 °C(Predicted)
  • 密度 :1.337±0.06 g/cm3(Predicted)
  • 储存条件 :Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
  • 溶解度 :DMSO: soluble5mg/mL, clear
  • 形态 :powder
  • 酸度系数(pKa) :15.08±0.30(Predicted)
  • 颜色 :yellow to brown
安全信息
  • 危险品标志 :Xn
  • 危险类别码 :22-36
  • 安全说明 :26
  • WGK Germany :3
  • 海关编码 :2933998090

2-氯-1-(1H-吲哚-3-基)-乙酮性质、用途与生产工艺

  • 生物活性 3CAI 是一种有效的特异性 AKT1 和 AKT2 抑制剂。
  • 靶点

    Akt1

    Akt2

  • 体外研究

    3CAI is a potential inhibitor of AKT. Based on these screening data, the effect of 3CAI on the kinase activities of AKT1, MEK1, JNK1, ERK1 and TOPK is tested using in vitro kinase assays. The results show that 3CAI (1 μM) suppresses only AKT1 kinase activity and the other kinases tested are not affected by 3CAI. 3CAI is a much more potent AKT1 inhibitor than PI3K (60% inhibition at 1 vs 10 μM, respectively). 3CAI substantially suppresses AKT1 activity as well as AKT2 activity in a dose dependent manner. 3CAI inhibits down-stream targets of AKT and induces apoptosis. AKT-mediated phosphorlyation site of mTOR (Ser2448) and GSK3β (Ser9) are substantially decreased by 3CAI in a time-dependent manner. Furthermore, pro-apoptotic marker proteins p53 and p21 are also upregulated by 3CAI after 12 or 24 h of treatment. HCT116 and HT29 colon cancer cells are seeded on 6 cm dishes in 1% FBS/McCoy's 5A (HCT116) with 3CAI (4 μM), I3C or the AKT inhibitor and then incubated for 4 days. Results show that the number of apoptotic cells is significantly increased by 3CAI in HCT116 and HT29 colon cancer cells compared with untreated control cells.

  • 体内研究

    To examine the antitumor activity of 3CAI in vivo, HCT116 cancer cells are injected into the right flank of individual athymic nude mice. Mice are orally administered 3CAI at 20 or 30 mg/kg, I3C at 100 mg/kg, or vehicle 5 times a week for 21 days. Treatment of mice with 30 mg/kg of 3CAI significantly suppresses HCT116 tumor growth by 50% relative to the vehicle-treated group (p<0.05). Remarkably, mice seem to tolerate treatment with these doses of 3CAI without overt signs of toxicity or significant loss of body weight compared with vehicle-treated group. Expression of these AKT-target proteins is strongly suppressed by 30 mg/kg of 3CAI in tumor tissues.

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2-氯-1-(1H-吲哚-3-基)-乙酮 试剂级价格
  • 更新日期:2024/11/08
  • 产品编号:HY-16666
  • 产品名称:2-氯-1-(1H-吲哚-3-基)-乙酮 3CAI
  • CAS编号:28755-03-5
  • 包装:5mg
  • 价格:580元
  • 更新日期:2024/11/08
  • 产品编号:HY-16666
  • 产品名称:2-氯-1-(1H-吲哚-3-基)-乙酮 3CAI
  • CAS编号:28755-03-5
  • 包装:10mM * 1mLin DMSO
  • 价格:638元
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