- WYE-354
- GDC-0349
- LY 303511
- GDC-mTOR inhibitor
- Nordihydroguaiaretic acid
| AZD2014Novel mTOR inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- View current batch:
- Purity = 98.36%
- COA (Certificate Of Analysis)
- HPLC(Retest)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | AZD2014 is a novel inhibitor of mTOR with an IC50 value of 2.8 nM. | |||||
| Targets | mTOR | P-Akt (S473) | pS6 (S235/236) | |||
| IC50 | 2.8 nM | 80 nM | 200 nM | |||
| Cell experiment [1]: | |
Cell lines | HCCLM3, Huh-7, SMMC-7721 and HepG2 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | 10 nM ~ 20 mM; 72 hrs |
Applications | In 4 selected HCC cell lines, AZD2014 exhibited a more profound antiproliferative activity than Rapamycin, with the IC50 values of 101, 441, 141 and 600 nM, respectively. SMMC-7721 cells were resistant to Rapamycin (even at a high concentration of 20 μM), but were highly sensitive to AZD2014 (141 nM). |
References: [1]. Dramatic antitumor effects of the dual mTORC1 and mTORC2 inhibitor AZD2014 in hepatocellular carcinoma.Am J Cancer Res. 2014 Dec 15;5(1):125-39. eCollection 2015. | |
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| Cas No. | 1009298-59-2 | SDF | Download SDF |
| Synonyms | AZD 2014;AZD-2014 | ||
| Chemical Name | 3-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-N-methylbenzamide | ||
| Canonical SMILES | CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOCC5C | ||
| Formula | C25H30N6O3 | M.Wt | 462.54 |
| Solubility | ≥23.15mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AZD2014 is a novel, potent and highly selective dual inhibitor of the mammalian rapamycin (mTORC1 and mTORC2) with an IC50 value of 2.8 nM. It is an oral inhibitor and possesses potential antineoplastic activity.
AZD2014 enhanced susceptibility of glioblastoma stem-like cells (GSCs) to irradiation both in vitro and under orthotopic in vivo conditions. Kahn J et al pretreated CD133+ and CD15+ GSC cells with AZD2014 (2 µM) for 1 hour, followed by irradiation. The effect was then measured by clonogenic survival analysis [2]. Using in vitro screening, they demonstrated that the combination of ibrutinib, an inhibitor of the tyrosine kinase BTK, and AZD2014 could dramatically induce apoptosis in ABC-subtype DLBCL cell lines. Thereby, the combination of AZD2014 with a BTK inhibitor is a promising therapeutic method to cure patients with ABC-type DLBCL [3]. In hepatocellular carcinoma cells, AZD2014 gave rise to a more complete inhibition of mTORC1 than rapamycin, while the inhibition of mTORC2 prevented the feedback activation of AKT signaling. Therefore, AZD2014 was identified to be more efficacious in the induction of apoptosis, autophagy, and cell cycle arrest, resulting in a significant proliferation suppression of the cells, in contrast with rapamycin [4].
In a recent human pharmacokinetic and pharmacodynamic study, a dose of 50mg BD(twice a day)AZD2014 was recommended to achieve pharmacologically relevant plasma concentrations [5].
References:Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6. The mTORC1/mTORC2 inhibitor AZD2014 enhances the radiosensitivity of glioblastoma stem-like cells. Neuro Oncol. 2014 Jan;16(1):29-37. Synergistic induction of apoptosis by combination of BTK and dual mTORC1/2 inhibitors in diffuse large B cell lymphoma. Oncotarget. 2014 Jul 15;5(13):4990-5001.Dramatic antitumor effects of the dual mTORC1 and mTORC2 inhibitor AZD2014 in hepatocellular carcinoma. Am J Cancer Res. 2014 Dec 15;5(1):125-39. eCollection 2015.First-in-human pharmacokinetic and pharmacodynamic study of the dual m-TORC 1/2 inhibitor, AZD2014. Clin Cancer Res. 2015 Mar 24. pii: clincanres.2422.2014.
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实验室自己做滴丸，基质用的PEG4000和PEG6000混合，80℃在水浴锅上熔融，只要基质离开水浴锅就会冷凝，胶头滴管会堵住，滴不出来，是什么原因，怎么解决，各位大神看到帮帮忙
顺便说一下水浴锅内注多少水为为适宜，常规水浴锅注水应在整个内胆三分之二为适中，如水太少了，温度反冲偏大，会影响整机精度。太多了会溢出体外。说具体一点，水浴锅注水多少，这要在放入量杯，水不溢出体外即可。
参考资料:Hi.baidu/=。www.jingda17.net。DI
两者还是有区别的
，以下是水浴锅与水槽的用途介绍。
恒温水浴锅主要用于对需要加热的样品进行所需某一温度的精确控制，以实现在对不同样品在同一种温控环境下作出比较，或同一样品在不同温度下所呈现的不同状态进行比对。由于恒温水浴锅内的水处于静止状态，所以在不同点会产生较小的温度差异。水浴锅一般用于对容器（如烧杯等）的加热，
水浴锅是分孔的，有2孔，4孔，8孔等，烧杯孔可任意改变大小。
恒温水槽
恒温水槽的使用范围比较广，适用于生物、化学、医药、食品、化工、石油等领域作精密恒温试验
，和辅助加热制冷之用。恒温水槽结构为金属长方形，采用优质钢板精心制作外壳，不锈钢内胆，数显温控仪，电源，水泵均装在控制盒内，恒温槽有一个核心功能微机控制、自整定PID调节控温
，用来控制温度的变化，最终达到一个恒温的作用！
低温恒温浴槽也可以利用外循环功能，通过与其他设备连接的软管，将槽内受控的恒温液体引导到其他设备。低温恒温槽
