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AZD2014 化学構造
分子量: 462.54



Quality Control & MSDS




情報 AZD2014は、潜在的抗新生物性活動による新しい二重mTORC1とmTORC2阻害剤です。
目標 mTOR
IC50 2.8 nM [1]
In vitro試験 AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy. [1]
In vivo試験 AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates. [1]
臨床試験 AZD2014 is now under Phase 1 clinical trial to assess the safety, tolerability, pharmacokinetics and preliminary efficacy in advanced solid malignancies.

推薦された実験操作 (公開の文献だけ)




Download AZD2014 SDF
分子量 462.54


CAS No. 1009298-59-2
別名 N/A
溶解度 (25°C)
  • DMSO 38 mg/mL
  • 水 <1 mg/mL
  • エタノール <1 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide


カスタマーレビュー (4)

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Source Dr Milica Pesic from Institute for Biological Research. AZD2014 purchased from Selleck
Method Western blot
Cell Lines NCI-H460 cells /NCI-H460/R cells
Concentrations 100/250 nM
Incubation Time 18 h
Results Concentration-dependent cell growth inhibition induced by AZD2014 did not differ between sensitive (NCI-H460) and multi-drug resistant (NCI-H460/R) human non-small cell lung carcinoma cell lines (A). AZD2014 cell growth inhibition efficacy decreased in multi-drug resistant colorectal carcinoma cell line DLD1-TxR in comparison to its sensitive counterpart DLD1 (B). The results were obtained by the Sulforhodamine B assay. All values represent average ?SD obtained from two independent experiments, n = 5. (DLD1 possesses mutated p53, while its resistant counterpart DLD1-TxR additionally acquired the LOH in PTEN gene during the course of resistance induction.)

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Source , , Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. AZD2014 purchased from Selleck
Method FACS
Cell Lines HT-29 cells
Concentrations 50 nM
Incubation Time 72 h
Results HT-29 cells were treated with vehicle or AZD-2014 (50 nM) for 72 h, cell cycle distribution was analyzed by FACS. AZD-2014 could arrest cells in G2 and G0/G1 phases.

Click to enlarge
Source , , Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. AZD2014 purchased from Selleck
Method MTT
Cell Lines HT-29 cells
Concentrations 1-100 nM
Incubation Time 72 h
Results HT-29 cells were treated with vehicle ("Ctrl") or different concentrations of AZD-2014 for 72 h. AZD-2014 dose-dependently inhibited HT-29 cell growth.

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Source , , Dr Milica Pesic from Institute for Biological Research. AZD2014 purchased from Selleck
Cell Lines Sea urchin embryo
Incubation Time 24 h
Results The effects of SelleckChem inhibitors on sea urchin embryo development evaluated 24 h after fertilization. All compounds were added to embryos suspension 20 min after fertilization. The relative presence of late gastrula, swimming blastula, undeveloped embryos and dead embryos was compared next to untreated control embryos (A). Fertilized egg, swimming blastula and late gastrula are illustrated (B). The embryonic development was relatively synchronized in untreated control samples after 24 h (A, E). GSK690693 treatment sustained the development of embryos. Swimming blastulas kept normal motility regardless the deformities in their shape. Tipifarnib treatment induced significant toxicity due to occurrence of dead fragmented embryos. Some abnormal blastulas kept the motility. AZD2014 treatment sustained the development of embryos. Some developed gastrulas and blastulas were less motile in comparison with control (A, C). WZ811 was the least toxic compound. Significant number of gastrulas and blastulas was developed. However, their motility was considerably suppressed (A, D). In contrast to SelleckChem inhibitors, classic anticancer agent – cisplatin was extremely toxic to sea urchin embryos (A). Cisplatin killed many embryos, while a small amount of survived embryos was stopped at early phases of development: immediately after fertilization or after first and second division (A, F).

製品表彰状 (3)

  • Rapamycin Induces MAP Kinase Phosphatase (MKP)-1 Expression Through Activation of Protein Kinase B and Mitogen-activated Protein Kinase Kinase Pathways. [Rastogi R, et al. J Biol Chem 2013;288(47):33966-77]

    PubMed: 24126911
  • The dual mTORC1 and mTORC2 inhibitor AZD8055 inhibits head and neck squamous cell carcinoma cell growth in vivo and in vitro [Li Q,et al. Biochem Biophys Res Commun 2013;440(4):701-6]

    PubMed: 24103749
  • Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. [Huo HZ, et al. Biochem Biophys Res Commun 2013;443(2):406-12]

    PubMed: 24309100



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