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IC6230 3CAI 抑制剂/拮抗剂/激动剂 索莱宝

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  • ¥251 - 2590
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  • 北京
  • IC6230
  • 2025年12月23日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 保质期

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 英文名

      3CAI

    • 库存

      现询

    • 供应商

      北京索莱宝科技有限公司

    • CAS号

      28755-03-5

    • 规格

      50mg/25mg/10mg/1mg/5mg

    规格:50mg产品价格:¥2590.0
    规格:25mg产品价格:¥1615.0
    规格:10mg产品价格:¥849.0
    规格:1mg产品价格:¥251.0
    规格:5mg产品价格:¥570.0

    基本信息
    CASNo.28755-03-5
    英文名称3CAI
    别名;Ro4-2130;2-氯-1-(1H-吲哚-3-基)-乙酮;3-氯乙酰基吲哚;4-氨甲基苯磺酰胺盐酸盐;
    分子式C10H8ClNO
    分子量193.63
    溶解性Soluble in DMSO ≥10mg/mL(Need ultrasonic)
    纯度≥98%
    外观(性状)Off-white to pink Solid
    储存条件Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
    MDLMFCD00464796
    SMILESC1=CC=C2C(=C1)C(=CN2)C(=O)CCl
    InChIKeyLLZQFAXTCYDVTR-UHFFFAOYSA-N
    InChIInChI=1S/C10H8ClNO/c11-5-10(13)8-6-12-9-4-2-1-3-7(8)9/h1-4,6,12H,5H2
    PubChem CID152961
    靶点Akt1/2
    通路PI3K/Akt/mTOR
    背景说明3CAI 是一种有效的特异性 AKT1 和 AKT2 抑制剂。
    生物活性3CAI is a potent and specific AKT1 and AKT2 inhibitor.[1]
    In Vitro3CAI 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/McCoys 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[1].
    细胞实验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[1].
    细胞实验HCT116 or HCT29 colon cancer cells are plated into 60-mm culture dishes (1×105 cells/dish) and incubated for 1 day in medium containing 10% FBS. The culture medium is then replaced with a 1% serum medium and cultured for 4 days with 3CAI (4 μM), I3C or a commercial AKT inhibitor. The cells are collected by trypsinization and washed with phosphate buffered saline (PBS). The cells are resuspended in 200 μL of binding buffer. Annexin V staining is accomplished. The cells are observed under a fluorescence microscope using a dual filter set for FITC and propidium iodide and then analyzed by flow cytometry[1].
    动物实验Mice[1]
    Athymic mice [Cr:NIH(S), NIH Swiss nude, 6-9 wk old] are divided into five groups: 1) untreated vehicle group (n=15); 2) 20 mg 3CAI/kg of body weight (n=15), 3) 30 mg 3CAI/kg body weight (n=15); 4) 100 mg I3C/kg of body weight (n=15); 5) no cells and 30 mg 3CAI/kg of body weight (n=15). HCT116 cells (3×106 cells/100 μL) are suspended in serum free McCoys 5A medium and inoculated subcutaneously into the right flank of each mouse. 3CAI, I3C or vehicle is administered orally 5 times per week for 21 days. Tumor volume is calculated. Mice are monitored until tumors reach 1 cm3 total volume, at which time mice are euthanized and tumors are extracted.
    激酶实验The kinase assay is performed. Briefly, the reaction is carried out in the presence of 10 μCi of [γ-32P]ATP with each compound (e.g., 3CAI, 0.5, 1, 2 and 4 μM) in 40 μL of reaction buffer containing 20 mM HEPES (pH 7.4), 10 mM MgCl2, 10 mM MnCl2, and 1 mM dithiothreitol. After incubation at room temperature for 30 min, the reaction is stopped by adding 10 μL protein loading buffer and the mixture is separated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). The relative amounts of incorporated radioactivity are assessed by autoradiography[1].
    数据来源文献[1]. Kim DJ, et al. (3-Chloroacetyl)-indole, a novel allosteric AKT inhibitor, suppresses colon cancer growth in vitro and in vivo. Cancer Prev Res (Phila). 2011 Nov;4(11):1842-51.
    单位

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