AZD2014是高效mTOR抑制剂,IC50为2.8 nM,对PI3K各亚型(α/β/γ/δ)的抑制性较弱。
AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). Phase 2.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Sylvie M, et al, AACR Annual Meeting, 2012, Abst 917.
分子式 C25H30N6O3 |
分子量 462.54 |
CAS号 1009298-59-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 35 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT03061708 | Stomach Neoplasms | Drug: AZD2014 | Samsung Medical Center | Phase 2 | 2017-02-01 | 2017-02-21 |
NCT02193633 | Advanced Cancer | Drug: AZD2014 3 on/4 off & weekly paclitaxel|Drug: AZD2014 2 on/5 off & weekly paclitaxel | Royal Marsden NHS Foundation Trust|Institute of Cancer Research, United Kingdom|AstraZeneca | Phase 1 | 2013-04-01 | 2015-03-11 |
NCT02064608 | Prostate Cancer | Drug: AZD2014 | Cambridge University Hospitals NHS Foundation Trust|AstraZeneca | Phase 1 | 2014-10-01 | 2017-01-06 |
NCT01597388 | Advanced Metastatic Breast Cancer | Drug: AZD2014|Drug: Fulvestrant | AstraZeneca | Phase 1 | 2012-05-01 | 2017-01-23 |
NCT02619864 | Glioblastoma Multiforme | Drug: AZD2014 | Canadian Cancer Trials Group|AstraZeneca | Phase 1|Phase 2 | 2015-11-01 | 2017-03-13 |
NCT02780830 | Core: Relapsed or Refractory Diffuse Large B-Cell Lymphoma|Module 1: Non-GCB Diffuse Large B-Cell Lymphoma | Drug: AZD2014|Drug: Ibrutinib | AstraZeneca | Phase 1 | 2016-06-01 | 2016-09-14 |
NCT01026402 | Advanced Solid Malignancies | Drug: AZD2014 | AstraZeneca | Phase 1 | 2009-12-01 | 2016-01-13 |
NCT01793636 | Metastatic Clear Cell Renal Carcinoma | Drug: AZD2014|Drug: Everolimus | Queen Mary University of London|AstraZeneca|Cancer Research UK | Phase 2 | 2013-02-01 | 2014-06-23 |
NCT03071874 | Meningioma | Drug: AZD2014 | Massachusetts General Hospital|National Cancer Institute (NCI)|AstraZeneca | Phase 2 | 2017-03-15 | 2017-03-01 |
NCT02208375 | Breast Cancer|Malignant Female Reproductive System Neoplasm | Drug: Olaparib|Drug: AZD2014|Drug: AZD5363 | M.D. Anderson Cancer Center|AstraZeneca|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2014-11-01 | 2017-03-06 |
NCT02831257 | Neurofibromatosis 2|Meningioma | Drug: AZD2014 | Massachusetts General Hospital|AstraZeneca|United States Department of Defense | Phase 2 | 2016-07-01 | 2016-09-25 |
NCT02583542 | Triple-Negative Breast Cancer|Squamous Cell Lung Cancer|Non-squamous Cell Lung Cancer With KRAS Mutations|Non-squamous Cell Lung Cancer With Wild-type KRAS | Drug: AZD2014|Drug: AZD6244 | Queen Mary University of London|Cancer Research UK|AstraZeneca | Phase 1|Phase 2 | 2015-06-01 | 2015-10-20 |
NCT02403895 | Squamous Non Small Cell Lung Cancer | Drug: Open-label AZD2014|Drug: paclitaxel | AstraZeneca | Phase 2 | 2015-04-01 | 2017-01-27 |
NCT02398747 | Advanced Solid Malignancies | Drug: AZD2014 | AstraZeneca | Phase 1 | 2015-03-01 | 2017-02-27 |
NCT03082833 | Cancer of Stomach | Drug: AZD2014 | Samsung Medical Center | Phase 2 | 2017-02-01 | 2017-03-12 |
NCT02599714 | Advanced and Metastatic Breast Cancer | Drug: AZD2014|Drug: Placebo to match AZD2014|Drug: palbociclib|Drug: fulvestrant|Drug: Placebo to match palbociclib | AstraZeneca|SCRI Development Innovations, LLC | Phase 1|Phase 2 | 2015-12-01 | 2017-02-22 |
NCT02752204 | Diffuse Large B-Cell Lymphoma | Drug: AZD 2014|Drug: Rituximab | University of Birmingham|Bloodwise|AstraZeneca|Cancer Research UK | Phase 2 | 2015-10-01 | 2017-02-03 |
NCT02640755 | Solid Malignancies | Drug: [14C]AZD2014|Drug: Multiple dose AZD2014|Drug: Fulvestrant|Drug: Paclitaxel | AstraZeneca|Quintiles, Inc. | Phase 1 | 2016-01-01 | 2017-02-27 |
NCT02216786 | Estrogen Receptor Positive Breast Cancer | Drug: AZD2014|Drug: Everolimus|Drug: Fulvestrant | Queen Mary University of London|AstraZeneca | Phase 2 | 2014-01-01 | 2015-01-23 |
NCT02730923 | Endometrial Carcinoma|Metastatic Carcinoma|Hormone Receptor Positive Tumor | Drug: AZD2014|Drug: Anastrozole | Centre Leon Berard | Phase 1|Phase 2 | 2016-04-01 | 2016-11-02 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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