2-氯-1-(1H-吲哚-3-基)-乙酮
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- CAS号:
- 28755-03-5
- 英文名:
- Ethanone, 2-chloro-1-(3-indolyl)-
- 英文别名:
- 3CAI;3CAI >=95% (HPLC);3-chloroacetylindole;Akt Inhibitor XIX, 3CAI;Chloromethyl indol-3-yl ketone;3-(Chloroacetyl)-1H-indole 95%;2-Chloro-1-(3-Indolyl)-Ethanone;Ethanone, 2-chloro-1-(3-indolyl)-;Ethanone, 2-chloro-1H-indol-1-yl-;Ethanone, 2-chloro-1-(1H-indol-3-yl)-
- 中文名:
- 2-氯-1-(1H-吲哚-3-基)-乙酮
- 中文别名:
- 3-氯乙酰基吲哚;2-氯-1-(3-吲哚基)-乙酮;乙酮,2-氯-1H-吲哚-1-基-;乙酮,2-氯-1-(3-吲哚基)-;3CAI,AKT1 和 AKT2 抑制剂;2-氯-1-(1H-吲哚-3-基)-乙酮;乙酮,2-氯-1-(1H-吲哚-3-基)-
- CBNumber:
- CB41247653
- 分子式:
- C10H8ClNO
- 分子量:
- 193.63
- MOL File:
- 28755-03-5.mol
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2-氯-1-(1H-吲哚-3-基)-乙酮化学性质
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熔点:
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212-214 °C(Solv: ethyl ether (60-29-7))
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沸点:
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379.1±17.0 °C(Predicted)
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密度:
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1.337±0.06 g/cm3(Predicted)
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储存条件:
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Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
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溶解度:
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DMSO: soluble5mg/mL, clear
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形态:
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powder
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酸度系数(pKa):
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15.08±0.30(Predicted)
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颜色:
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yellow to brown
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2-氯-1-(1H-吲哚-3-基)-乙酮性质、用途与生产工艺
3CAI 是一种有效的特异性 AKT1 和 AKT2 抑制剂。
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.
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.
2-氯-1-(1H-吲哚-3-基)-乙酮
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/11/08 | HY-16666 | 2-氯-1-(1H-吲哚-3-基)-乙酮
3CAI | 28755-03-5 | 5mg | 580元 |
| 2024/11/08 | HY-16666 | 2-氯-1-(1H-吲哚-3-基)-乙酮
3CAI | 28755-03-5 | 10mM * 1mLin DMSO | 638元 |
2-氯-1-(1H-吲哚-3-基)-乙酮
生产厂家
28755-03-5, 2-氯-1-(1H-吲哚-3-基)-乙酮 相关搜索:
- 抑制剂
- 高端化学
- 3CAI,AKT1 和 AKT2 抑制剂
- 2-氯-1-(1H-吲哚-3-基)-乙酮
- 3-氯乙酰基吲哚
- 乙酮,2-氯-1H-吲哚-1-基-
- 乙酮,2-氯-1-(3-吲哚基)-
- 乙酮,2-氯-1-(1H-吲哚-3-基)-
- 2-氯-1-(3-吲哚基)-乙酮
- 28755-03-5
- Inhibitor,3CAI,inhibit,Akt,Protein kinase B,PKB
- 3CAI >=95% (HPLC)
- 3-(Chloroacetyl)-1H-indole 95%
- Akt Inhibitor XIX, 3CAI - CAS 28755-03-5 - Calbiochem
- Akt Inhibitor XIX, 3CAI
- 2-Chloro-1-(3-Indolyl)-Ethanone
- Ethanone, 2-chloro-1H-indol-1-yl-
- Ethanone, 2-chloro-1-(1H-indol-3-yl)-
- Chloromethyl indol-3-yl ketone
- 3CAI
- 2-Chloro-1-(1H-indol-3-yl)ethan-1-one, 3-(2-Chloroethanoyl)-1H-indole
- 2-chloro-1-(1H-indol-3-yl)ethanone(SALTDATA: FREE)
- 3-chloroacetylindole
- Ethanone, 2-chloro-1-(3-indolyl)-