Apatinib是一种口服生物有效性的VEGFR2选择性抑制剂,IC50为1 nM。
Apatinib (YN968D1)is a potent inhibior of the VEGF signaling pathway with the IC50 value of 1nM for VEGFR-2 in in vitro enzyme experiments.
50, 100, 200 mg/kg 口服
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] Tian S, et al. Cancer Sci, 2011, 102(7), 1374-1380.
分子式 C25H27N5O4S |
分子量 493.58 |
CAS号 811803-05-1(1218779-75-9) |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 20 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 |
NCT02836821 | Neoplasms | Drug: Apatinib Mesylate Tablets|Drug: Rifampicin Capsules | Jiangsu HengRui Medicine Co., Ltd. | Phase 1 | 2016-05-01 | 2017-02-23 |
NCT02995187 | Small Cell Lung Cancer | Drug: Apatinib Mesylate tablet | Chinese Academy of Medical Sciences | Phase 2 | 2016-12-01 | 2016-12-14 |
NCT02829385 | Colorectal Neoplasms | Drug: Apatinib and XELOX combined treatment group | Shoucheng Ma|LanZhou University | Phase 2 | 2016-06-01 | 2016-07-11 |
NCT02544737 | Esophageal Cancer|Metastatic Esophageal Cancer|Apatinib | Drug: Apatinib | Hangzhou Cancer Hospital | Phase 2 | 2015-09-01 | 2016-08-25 |
NCT02772029 | Hepatocellular Carcinoma | Drug: Apatinib Mesylate Tablets | The First Affiliated Hospital of Zhengzhou University | Phase 1|Phase 2 | 2016-05-01 | 2016-05-12 |
NCT02515435 | Non-Small Cell Lung Cancer | Drug: apatinib single agent | Tongji University | Phase 2 | 2015-01-01 | 2015-07-31 |
NCT02540824 | Non-small Cell Lung Cancer | Drug: Apatinib single agent arm | Tongji University | Phase 2 | 2015-01-01 | 2015-09-03 |
NCT02726854 | Pancreatic Neoplasms | Drug: Apatinib | First Affiliated Hospital Xi'an Jiaotong University | Phase 2 | 2016-04-01 | 2016-11-30 |
NCT03046979 | Hepatocellular Carcinoma | Drug: Apatinib | Tianjin Medical University Cancer Institute and Hospital | Phase 2 | 2016-12-01 | 2017-02-06 |
NCT02836171 | Neoplasms | Drug: Apatinib Mesylate Tablets|Drug: Itraconazole Capsules | Jiangsu HengRui Medicine Co., Ltd. | Phase 1 | 2016-07-01 | 2017-02-23 |
NCT03083041 | Carcinoma, Non-Small-Cell Lung | Biological: SHR-1210|Drug: Apatinib | Jiangsu HengRui Medicine Co., Ltd. | Phase 2 | 2017-03-01 | 2017-03-13 |
NCT02989259 | Head and Neck Neoplasms | Drug: Apatinib | Cancer Institute and Hospital, Chinese Academy of Medical Sciences | Phase 2 | 2016-12-01 | 2016-12-11 |
NCT02485015 | Stomach Neoplasms | Biological: Cytokine-Induced Killer Cells|Drug: Apatinib | The First People's Hospital of Changzhou | Phase 2 | 2015-06-01 | 2016-02-18 |
NCT02493582 | Adenocarcinoma of Lung | Biological: Cytokine-Induced Killer Cells|Drug: Apatinib | The First People's Hospital of Changzhou | Phase 2 | 2015-07-01 | 2016-02-04 |
NCT01653561 | Breast Neoplasms | Drug: Apatinib | Fudan University|Jiangsu HengRui Medicine Co., Ltd. | Phase 2 | 2011-11-01 | 2013-12-02 |
NCT02878057 | Breast Cancer | Drug: Apatinib | Beijing Cancer Hospital|Hebei Medical University Fourth Hospital|Peking University First Hospital|Peking University Third Hospital|Shanxi Province Cancer Hospital | Phase 2 | 2016-05-01 | 2016-08-24 |
NCT03007446 | Gastric Cancer | Drug: Apatinib|Drug: Oxaliplatin|Drug: S-1 | Chinese PLA General Hospital | Phase 2 | 2016-11-01 | 2016-12-29 |
NCT02537171 | Gastric Cancer | Drug: apatinib | The Affiliated Hospital of the Chinese Academy of Military Medical Sciences | Phase 3 | 2015-07-01 | 2016-08-01 |
NCT02711007 | Osteosarcoma|Metastasis | Drug: apatinib | GUO WEI|Peking University People's Hospital | Phase 2|Phase 3 | 2016-03-01 | 2016-03-16 |
NCT02774200 | Metastatic Renal Cell Carcinoma | Drug: Apatinib | Tianjin Medical University Cancer Institute and Hospital | Phase 2 | 2016-05-01 | 2016-05-12 |
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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