1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. VEGFR
    Autophagy

Apatinib (Synonyms: YN968D1)

Cat. No.: HY-13342 Purity: 99.76%
Data Sheet SDS Handling Instructions

Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib has no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM.

For research use only. We do not sell to patients.
Apatinib Chemical Structure

Apatinib Chemical Structure

CAS No. : 1218779-75-9

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  • Biological Activity

  • Protocol

  • Technical Information

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Description

Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib has no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM.

IC50 & Target

IC50: 1 nM (VEGFR2), 13 nM (Ret), 429 nM (c-Kit), 530 nM (c-Src)[1]

In Vitro

Apatinib (YN968D1) slightly inhibits proliferation of HUVEC stimulated by 20% FBS (IC50=23.4 μM), whereas Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50=0.17 μM). The IC50 values of Sunitinib are lower under the same conditions (7.4 μM and 0.034 μM, respectively). 1 μM Apatinib significantly inhibits the migration of HUVEC induced by FBS, but does not affect proliferation of HUVEC, indicating that the inhibitory effect of Apatinib on FBS-induced migration is not due to the suppression of proliferation. At a concentration of 1 μM, Sunitinib also inhibits the migration of HUVEC[1].

In Vivo

The antitumor potential of Apatinib (YN968D1) is evaluated in six human tumor xenografts in immunodeficient mice. Once-daily oral administration of Apatinib produces a dose-dependent inhibition of tumor growth in all tumor models examined. Statistically significant growth inhibition is obtained with 50 mg/kg per day Apatinib in three of five tumor xenografts tested. Each tumor xenograft model is significantly growth inhibited by Apatinib at the dose of 100 kg/day. Similar tumor growth inhibition is observed (T/C%, 8% to 18%) in mice following treatment with Apatinib at the dose of 200 kg/day. Full growth inhibition profiles are shown for three of the xenografts. Compared with the control animals, no effect of Apatinib treatment on bodyweight is observed at any dose level, which suggested that Apatinib is well tolerated[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT03121846 Tianjin Medical University Cancer Institute and Hospital|Zhejiang Cancer Hospital|Gansu Cancer Hospital|Liaoning Tumor Hospital & Institute|Fudan University Soft Tissue Sarcoma, Adult, Stage II May 1, 2017 Phase 2
NCT02836821 Jiangsu HengRui Medicine Co., Ltd. Neoplasms May 2016 Phase 1
NCT02995187 Chinese Academy of Medical Sciences Small Cell Lung Cancer December 2016 Phase 2
NCT03064243 Shanghai Jiao Tong University Affiliated Sixth People’s Hospital Soft Tissue Sarcoma March 1, 2017 Phase 2
NCT03020979 First Affiliated Hospital Bengbu Medical College Malignant Ascites|Apatinib January 2017 Phase 2
NCT02829385 Shoucheng Ma|LanZhou University Colorectal Neoplasms June 2016 Phase 2
NCT02544737 Hangzhou Cancer Hospital Esophageal Cancer|Metastatic Esophageal Cancer|Apatinib September 2015 Phase 2
NCT03228043 Nanchong Central Hospital Apatinib|Outcome, Fatal|Colorectal Cancer|Surgery|Adjuvant Chemotherapy August 1, 2017
NCT03144856 Sun Yat-sen University|Jiangsu HengRui Medicine Co., Ltd. Biliary Tract Cancer February 22, 2017 Phase 2
NCT03180476 Sichuan Cancer Hospital and Research Institute|Jiangsu HengRui Medicine Co., Ltd. Nasopharyngeal Neoplasms April 1, 2017 Phase 2
NCT03129256 Changzhou Cancer Hospital of Soochow University Non-small Cell Lung Cancer December 1, 2016 Phase 2
NCT02772029 The First Affiliated Hospital of Zhengzhou University Hepatocellular Carcinoma May 2016 Phase 1|Phase 2
NCT02515435 Tongji University Non-Small Cell Lung Cancer January 2015 Phase 2
NCT02540824 Tongji University Non-small Cell Lung Cancer January 2015 Phase 2
NCT02726854 First Affiliated Hospital Xi'an Jiaotong University Pancreatic Neoplasms April 2016 Phase 2
NCT03046979 Tianjin Medical University Cancer Institute and Hospital Hepatocellular Carcinoma December 2016 Phase 2
NCT03190616 The First Affiliated Hospital with Nanjing Medical University|Jiangsu HengRui Medicine Co., Ltd.|Beijing gene plus technology co., LTD Colorectal Neoplasms July 1, 2017 Phase 2
NCT02836171 Jiangsu HengRui Medicine Co., Ltd. Neoplasms July 2016 Phase 1
NCT03083041 Jiangsu HengRui Medicine Co., Ltd. Carcinoma, Non-Small-Cell Lung March 2017 Phase 2
NCT03104335 Peking University People's Hospital|Peking University Shougang Hospital|Peking University International Hospital Soft Tissue Sarcoma Adult|Advanced Cancer April 1, 2017 Phase 2
NCT03193814 Wuhan Union Hospital, China Colorectal Cancer|Chemotherapy|Angiogenesis August 1, 2017 Phase 2
NCT03199677 Chinese Academy of Medical Sciences Refractory Cancer July 1, 2017 Phase 2
NCT02989259 Cancer Institute and Hospital, Chinese Academy of Medical Sciences Head and Neck Neoplasms December 2016 Phase 2
NCT02485015 The First People's Hospital of Changzhou Stomach Neoplasms June 2015 Phase 2
NCT02493582 The First People's Hospital of Changzhou Adenocarcinoma of Lung July 2015 Phase 2
NCT03129698 Junling Li|Peking Union Medical College Apatinib in Maintenance Treatment April 11, 2017 Phase 2
NCT03104283 Affiliated Hospital of Qinghai University Gastric Cancer June 2017 Phase 2
NCT03219593 First Affiliated Hospital Bengbu Medical College Gastric Cancer|Apatinib|Biomarker August 2017 Phase 2
NCT01653561 Fudan University|Jiangsu HengRui Medicine Co., Ltd. Breast Neoplasms November 2011 Phase 2
NCT02878057 Beijing Cancer Hospital|Hebei Medical University Fourth Hospital|Peking University First Hospital|Peking University Third Hospital|Shanxi Province Cancer Hospital Breast Cancer May 2016 Phase 2
NCT03007446 Chinese PLA General Hospital Gastric Cancer November 2016 Phase 2
NCT02537171 The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Gastric Cancer July 2015 Phase 3
NCT02711007 GUO WEI|Peking University People's Hospital Osteosarcoma|Metastasis March 2016 Phase 2|Phase 3
NCT02774200 Tianjin Medical University Cancer Institute and Hospital Metastatic Renal Cell Carcinoma May 2016 Phase 2
NCT03229096 Shanghai Zhongshan Hospital Chemotherapy Effect|Chemotherapeutic Toxicity|Gastric Cancer February 1, 2017 Phase 2
NCT02645864 Peking University|Jiangsu HengRui Medicine Co., Ltd. Esophageal Squamous Cell Carcinoma January 2016 Phase 1
NCT03132025 Yanqiao Zhang|Harbin Medical University Metastatic Colorectal Cancer April 30, 2017 Phase 2
NCT02727309 Beijing Cancer Hospital|Jiangsu HengRui Medicine Co., Ltd. Hepatocellular Carcinoma October 2015 Phase 1|Phase 2
NCT03029013 Third Military Medical University Cervical Cancer January 2017
NCT03210064 Hui ting Xu,MD|Jiangsu HengRui Medicine Co., Ltd.|Hubei Cancer Hospital Metastatic Colorectal Cancer May 4, 2017 Phase 2
NCT02844881 The First People's Hospital of Lianyungang|HengRui YuanZheng Bio-Technology Co.,Ltd. Advanced Solid Tumors|Excluding T Cell Lymphoma July 2016 Phase 1|Phase 2
NCT02874651 Sun Yat-sen University|First People's Hospital of Foshan|Guilin Medical University, China Nasopharyngeal Neoplasms October 2016 Phase 2
NCT03163381 Henan Cancer Hospital|Jiangsu HengRui Medicine Co., Ltd. Osteosarcoma, Advanced April 11, 2017 Phase 2
NCT03071042 Sir Run Run Shaw Hospital|Jiangsu HengRui Medicine Co., Ltd. Metastatic Gastric Adenocarcinoma October 2015 Phase 1
NCT02731352 Peking Union Medical College Hospital Thyroid Cancer February 2016 Phase 2
NCT01192971 Jiangsu HengRui Medicine Co., Ltd.|Eighty-One Hospital of People's Liberation Army Advanced Hepatocellular Carcinoma June 2010 Phase 2
NCT02711969 Bukwang Pharmaceutical Gastric Cancer March 2016 Phase 1
NCT03167385 Tianjin Medical University Cancer Institute and Hospital Differentiated Thyroid Carcinoma March 22, 2017 Phase 2
NCT00633490 Fudan University Tumor July 2007 Phase 1
NCT02824458 Sun Yat-sen University EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors June 2016 Phase 3
NCT02775370 Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University Adenoid Cystic Carcinoma June 2016 Phase 2
NCT02976896 Yuhong Li|Sun Yat-sen University Esophageal Squamous Cell Carcinoma August 2016 Phase 2
NCT02733107 Third Military Medical University Non-small Cell Lung Cancer March 2016 Phase 2
NCT03224221 The First Affiliated Hospital of Anhui Medical University Esophageal Squamous Cell Carcinoma March 23, 2017 Phase 2
NCT03086785 Hebei Medical University Fourth Hospital Breast Cancer Metastatic November 24, 2016 Phase 2
NCT02683655 Huai'an First People's Hospital|Jiangsu HengRui Medicine Co., Ltd. Esophageal Cancer August 2015 Phase 2
NCT02942693 Shanghai Proton and Heavy Ion Center Adenoid Cystic Carcinoma November 2016 Phase 2
NCT02426034 Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer February 2015 Phase 4
NCT02848794 The First People's Hospital of Lianyungang|Shandong Cancer Hospital and Institute|The Affiliated Hospital of Medical College of Qingdao University|Yankuang Group General Hospital|Lianyungang Hospital Affiliated Bengbu Medical College|Suzhou Kowloon Hospital High-grade Glioma July 2016 Phase 1|Phase 2
NCT02974933 Wuling Ou|Jiangsu HengRui Medicine Co., Ltd.|Hubei Clinical Research Collaboration Group|Hubei Cancer Hospital Nonsmall Cell Lung Cancer November 2016 Phase 2
NCT02867956 Sun Yat-sen University Ovarian Cancer August 2016 Phase 2
NCT03135977 Sichuan Cancer Hospital and Research Institute Extensive-stage Small Cell Lung Cancer|Lung Cancer March 1, 2017 Phase 2
NCT01176669 Fudan University|Jiangsu HengRui Medicine Co., Ltd. Metastatic Breast Cancer June 2010 Phase 2
NCT02943252 Cancer Institute and Hospital, Chinese Academy of Medical Sciences Head and Neck Neoplasms October 2016 Phase 2
NCT03130270 Guilin Medical University, China|Wuzhou Red Cross Hospital|Guangxi Naxishan Hospital|National Hospital of Guangxi Zhuang Autonomous Region Nasopharyngeal Carcinoma January 1, 2017 Phase 2
NCT02863367 Tianjin Medical University Cancer Institute and Hospital Metastatic Pancreatic Cancer August 2016 Phase 2
NCT03048877 Peking Union Medical College Hospital Differentiated Thyroid Cancer December 2016 Phase 3
NCT02942329 The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Gastric Cancer|Hepatocellular Carcinoma October 2016 Phase 1|Phase 2
NCT02691871 Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Jiangsu HengRui Medicine Co., Ltd. Lung Adenocarcinoma February 2016 Phase 1
NCT02525237 Qingdao Municipal Hospital|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer August 2015 Phase 2
NCT02780778 Tianjin Medical University Cancer Institute and Hospital Non-small Cell Lung Cancer May 2016 Phase 2|Phase 3
NCT01270386 Jiangsu HengRui Medicine Co., Ltd.|Sun Yat-sen University Non-Small-Cell Lung Cancer March 2010 Phase 2
NCT02409199 Shanghai Zhongshan Hospital Gastric Carcinoma June 2015 Phase 2|Phase 3
NCT03144843 Sun Yat-sen University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer January 13, 2017 Phase 2
NCT03114085 First Affiliated Hospital of Guangxi Medical University Hepatocellular Carcinoma May 20, 2017 Phase 2
NCT03050411 Peking University Third Hospital Nonsmall Cell Lung Cancer May 2016 Phase 1
NCT02702323 Zhejiang Cancer Hospital|First Affiliated Hospital of Zhejiang University|Second Affiliated Hospital, School of Medicine, Zhejiang University|The Central Hospital of Lishui City|First Affiliated Hospital of Wenzhou Medical Univeristy|Ningbo No.2 Hospital Hepatocellular Carcinoma|Pulmonary Metastasis March 2016 Phase 2|Phase 3
NCT02945852 Zhejiang Cancer Hospital Small Cell Lung Cancer October 2016 Phase 2
NCT03190239 Xinqiao Hospital of Chongqing Advanced Non-squamous Non-small-cell Lung Cancer July 15, 2017 Phase 2
NCT03075462 Jiangsu HengRui Medicine Co., Ltd.|Beijing Cancer Hospital Ovarian Cancer|Triple Negative Breast Cancer March 9, 2017 Phase 1
NCT03116555 China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region Metastatic Gastric Adenocarcinoma April 5, 2017 Phase 2
NCT02768415 Chinese Academy of Medical Sciences Breast Cancer June 2016 Phase 2
NCT02697838 Fujian Cancer Hospital Malignant Neoplasm of Stomach Stage II August 2016
NCT03066557 Jiangsu Cancer Institute & Hospital|Jiangsu HengRui Medicine Co., Ltd. Hepatocellular Carcinoma March 15, 2017
NCT02776527 Tianjin Medical University Cancer Institute and Hospital Gastric Cancer April 2016 Phase 4
NCT02332512 Jiangsu HengRui Medicine Co., Ltd. Carcinoma, Non-Small-Cell Lung January 2015 Phase 3
NCT00970138 Fudan University Gastric Carcinoma June 2009 Phase 2|Phase 3
NCT02764268 Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer June 2016
NCT02529878 The First Affiliated Hospital of Zhejiang Chinese Medical University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer August 2015 Phase 2
NCT01287962 Sun Yat-sen University Non-small Cell Lung Cancer April 2011 Phase 3
NCT03030937 Fujian Cancer Hospital Advanced Gastric Cancer Adenocarcinoma of Esophagogastric Junction February 1, 2017 Phase 2
NCT03213587 Zhejiang Cancer Hospital Nasopharyngeal Carcinoma July 1, 2017 Phase 2
NCT03127319 Affiliated Hospital of Hebei University Non-squamous Non-small Cell Lung Cancer May 2017 Phase 2
NCT03170310 Henan Cancer Hospital|Jiangsu HengRui Medicine Co., Ltd. Advanced Esophagus Cancer February 21, 2017 Phase 2
NCT03100955 Qingdao University Progression Free Survival March 1, 2017 Phase 3
NCT02875457 Third Military Medical University Small Cell Lung Cancer September 2016 Phase 3
NCT03164694 Sun Yat-sen University Lung Cancer May 20, 2017 Phase 2
NCT01512745 Jiangsu HengRui Medicine Co., Ltd.|Fudan University|The 81 Hospital of PLA Advanced or Metastatic Gastric Cancer January 2011 Phase 3
NCT03042611 LSK BioPartners Inc. Gastric Cancer|Gastric Adenocarcinoma February 24, 2017 Phase 3
NCT02596256 Chinese PLA General Hospital Gastric Cancer April 2016 Phase 2
NCT03096184 Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University Head and Neck Squamous Cell Carcinoma May 1, 2017 Phase 2
NCT02980809 First Hospitals affiliated to the China PLA General Hospital Small Cell Lung Cancer March 2017 Phase 2
NCT01531777 Jiangsu HengRui Medicine Co., Ltd.|Fudan University Colorectal Cancer April 2011 Phase 2
NCT03201146 West China Hospital|Jiangsu HengRui Medicine Co., Ltd. Lung Cancer|Non Small Cell Lung Cancer|Combination Chemotherapy|Apatinib June 27, 2017 Phase 1|Phase 2
NCT03192735 Chang-Ming Huang, Prof.|Fujian Medical University Safety and Effectiveness of Apatinib Combined With SOX Neoadjuvant Chemotherapy for Locally Advanced Gastric Cancer July 1, 2017 Phase 2
NCT02510469 Hebei Medical University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer July 2015 Phase 2|Phase 3
NCT03193424 The First Affiliated Hospital of Zhengzhou University Advanced Esophageal Squamous Carcinoma October 2016 Phase 2
NCT02509806 Hebei Medical University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer July 2015 Phase 2|Phase 3
NCT02852798 Jiangsu ShengDiYa Medicine Co., Ltd.|Dongguan People's Hospital Nonsquamous Nonsmall Cell Neoplasm of Lung August 2016
NCT02998242 Sichuan Provincial People's Hospital|Chang An Hospital|Hainan Medical College Quality of Life May 2016
NCT02329860 Jiangsu HengRui Medicine Co., Ltd.|NanJing PLA 81 Hospital Carcinoma, Hepatocellular January 13, 2014 Phase 3
NCT03092895 Jiangsu HengRui Medicine Co., Ltd. Advanced Primary Liver Cancer April 27, 2017 Phase 2
NCT03026881 Jiangsu HengRui Medicine Co., Ltd.|The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Recurrent and Metastatic Gastric Cancer January 2017 Phase 1
NCT02704767 The First Affiliated Hospital of Kunming Medical College Lung Cancer June 2016 Phase 2
NCT03121846 Tianjin Medical University Cancer Institute and Hospital|Zhejiang Cancer Hospital|Gansu Cancer Hospital|Liaoning Tumor Hospital & Institute|Fudan University Soft Tissue Sarcoma, Adult, Stage II May 1, 2017 Phase 2
NCT02836821 Jiangsu HengRui Medicine Co., Ltd. Neoplasms May 2016 Phase 1
NCT02995187 Chinese Academy of Medical Sciences Small Cell Lung Cancer December 2016 Phase 2
NCT03064243 Shanghai Jiao Tong University Affiliated Sixth People’s Hospital Soft Tissue Sarcoma March 1, 2017 Phase 2
NCT03020979 First Affiliated Hospital Bengbu Medical College Malignant Ascites|Apatinib January 2017 Phase 2
NCT02829385 Shoucheng Ma|LanZhou University Colorectal Neoplasms June 2016 Phase 2
NCT02544737 Hangzhou Cancer Hospital Esophageal Cancer|Metastatic Esophageal Cancer|Apatinib September 2015 Phase 2
NCT03228043 Nanchong Central Hospital Apatinib|Outcome, Fatal|Colorectal Cancer|Surgery|Adjuvant Chemotherapy August 1, 2017
NCT03144856 Sun Yat-sen University|Jiangsu HengRui Medicine Co., Ltd. Biliary Tract Cancer February 22, 2017 Phase 2
NCT03180476 Sichuan Cancer Hospital and Research Institute|Jiangsu HengRui Medicine Co., Ltd. Nasopharyngeal Neoplasms April 1, 2017 Phase 2
NCT03129256 Changzhou Cancer Hospital of Soochow University Non-small Cell Lung Cancer December 1, 2016 Phase 2
NCT02772029 The First Affiliated Hospital of Zhengzhou University Hepatocellular Carcinoma May 2016 Phase 1|Phase 2
NCT02515435 Tongji University Non-Small Cell Lung Cancer January 2015 Phase 2
NCT02540824 Tongji University Non-small Cell Lung Cancer January 2015 Phase 2
NCT02726854 First Affiliated Hospital Xi'an Jiaotong University Pancreatic Neoplasms April 2016 Phase 2
NCT03046979 Tianjin Medical University Cancer Institute and Hospital Hepatocellular Carcinoma December 2016 Phase 2
NCT03190616 The First Affiliated Hospital with Nanjing Medical University|Jiangsu HengRui Medicine Co., Ltd.|Beijing gene plus technology co., LTD Colorectal Neoplasms July 1, 2017 Phase 2
NCT02836171 Jiangsu HengRui Medicine Co., Ltd. Neoplasms July 2016 Phase 1
NCT03083041 Jiangsu HengRui Medicine Co., Ltd. Carcinoma, Non-Small-Cell Lung March 2017 Phase 2
NCT03104335 Peking University People's Hospital|Peking University Shougang Hospital|Peking University International Hospital Soft Tissue Sarcoma Adult|Advanced Cancer April 1, 2017 Phase 2
NCT03193814 Wuhan Union Hospital, China Colorectal Cancer|Chemotherapy|Angiogenesis August 1, 2017 Phase 2
NCT03199677 Chinese Academy of Medical Sciences Refractory Cancer July 1, 2017 Phase 2
NCT02989259 Cancer Institute and Hospital, Chinese Academy of Medical Sciences Head and Neck Neoplasms December 2016 Phase 2
NCT02485015 The First People's Hospital of Changzhou Stomach Neoplasms June 2015 Phase 2
NCT02493582 The First People's Hospital of Changzhou Adenocarcinoma of Lung July 2015 Phase 2
NCT03129698 Junling Li|Peking Union Medical College Apatinib in Maintenance Treatment April 11, 2017 Phase 2
NCT03104283 Affiliated Hospital of Qinghai University Gastric Cancer June 2017 Phase 2
NCT03219593 First Affiliated Hospital Bengbu Medical College Gastric Cancer|Apatinib|Biomarker August 2017 Phase 2
NCT01653561 Fudan University|Jiangsu HengRui Medicine Co., Ltd. Breast Neoplasms November 2011 Phase 2
NCT02878057 Beijing Cancer Hospital|Hebei Medical University Fourth Hospital|Peking University First Hospital|Peking University Third Hospital|Shanxi Province Cancer Hospital Breast Cancer May 2016 Phase 2
NCT03007446 Chinese PLA General Hospital Gastric Cancer November 2016 Phase 2
NCT02537171 The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Gastric Cancer July 2015 Phase 3
NCT02711007 GUO WEI|Peking University People's Hospital Osteosarcoma|Metastasis March 2016 Phase 2|Phase 3
NCT02774200 Tianjin Medical University Cancer Institute and Hospital Metastatic Renal Cell Carcinoma May 2016 Phase 2
NCT03229096 Shanghai Zhongshan Hospital Chemotherapy Effect|Chemotherapeutic Toxicity|Gastric Cancer February 1, 2017 Phase 2
NCT02645864 Peking University|Jiangsu HengRui Medicine Co., Ltd. Esophageal Squamous Cell Carcinoma January 2016 Phase 1
NCT03132025 Yanqiao Zhang|Harbin Medical University Metastatic Colorectal Cancer April 30, 2017 Phase 2
NCT02727309 Beijing Cancer Hospital|Jiangsu HengRui Medicine Co., Ltd. Hepatocellular Carcinoma October 2015 Phase 1|Phase 2
NCT03029013 Third Military Medical University Cervical Cancer January 2017
NCT03210064 Hui ting Xu,MD|Jiangsu HengRui Medicine Co., Ltd.|Hubei Cancer Hospital Metastatic Colorectal Cancer May 4, 2017 Phase 2
NCT02844881 The First People's Hospital of Lianyungang|HengRui YuanZheng Bio-Technology Co.,Ltd. Advanced Solid Tumors|Excluding T Cell Lymphoma July 2016 Phase 1|Phase 2
NCT02874651 Sun Yat-sen University|First People's Hospital of Foshan|Guilin Medical University, China Nasopharyngeal Neoplasms October 2016 Phase 2
NCT03163381 Henan Cancer Hospital|Jiangsu HengRui Medicine Co., Ltd. Osteosarcoma, Advanced April 11, 2017 Phase 2
NCT03071042 Sir Run Run Shaw Hospital|Jiangsu HengRui Medicine Co., Ltd. Metastatic Gastric Adenocarcinoma October 2015 Phase 1
NCT02731352 Peking Union Medical College Hospital Thyroid Cancer February 2016 Phase 2
NCT01192971 Jiangsu HengRui Medicine Co., Ltd.|Eighty-One Hospital of People's Liberation Army Advanced Hepatocellular Carcinoma June 2010 Phase 2
NCT02711969 Bukwang Pharmaceutical Gastric Cancer March 2016 Phase 1
NCT03167385 Tianjin Medical University Cancer Institute and Hospital Differentiated Thyroid Carcinoma March 22, 2017 Phase 2
NCT00633490 Fudan University Tumor July 2007 Phase 1
NCT02824458 Sun Yat-sen University EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors June 2016 Phase 3
NCT02775370 Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University Adenoid Cystic Carcinoma June 2016 Phase 2
NCT02976896 Yuhong Li|Sun Yat-sen University Esophageal Squamous Cell Carcinoma August 2016 Phase 2
NCT02733107 Third Military Medical University Non-small Cell Lung Cancer March 2016 Phase 2
NCT03224221 The First Affiliated Hospital of Anhui Medical University Esophageal Squamous Cell Carcinoma March 23, 2017 Phase 2
NCT03086785 Hebei Medical University Fourth Hospital Breast Cancer Metastatic November 24, 2016 Phase 2
NCT02683655 Huai'an First People's Hospital|Jiangsu HengRui Medicine Co., Ltd. Esophageal Cancer August 2015 Phase 2
NCT02942693 Shanghai Proton and Heavy Ion Center Adenoid Cystic Carcinoma November 2016 Phase 2
NCT02426034 Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer February 2015 Phase 4
NCT02848794 The First People's Hospital of Lianyungang|Shandong Cancer Hospital and Institute|The Affiliated Hospital of Medical College of Qingdao University|Yankuang Group General Hospital|Lianyungang Hospital Affiliated Bengbu Medical College|Suzhou Kowloon Hospital High-grade Glioma July 2016 Phase 1|Phase 2
NCT02974933 Wuling Ou|Jiangsu HengRui Medicine Co., Ltd.|Hubei Clinical Research Collaboration Group|Hubei Cancer Hospital Nonsmall Cell Lung Cancer November 2016 Phase 2
NCT02867956 Sun Yat-sen University Ovarian Cancer August 2016 Phase 2
NCT03135977 Sichuan Cancer Hospital and Research Institute Extensive-stage Small Cell Lung Cancer|Lung Cancer March 1, 2017 Phase 2
NCT01176669 Fudan University|Jiangsu HengRui Medicine Co., Ltd. Metastatic Breast Cancer June 2010 Phase 2
NCT02943252 Cancer Institute and Hospital, Chinese Academy of Medical Sciences Head and Neck Neoplasms October 2016 Phase 2
NCT03130270 Guilin Medical University, China|Wuzhou Red Cross Hospital|Guangxi Naxishan Hospital|National Hospital of Guangxi Zhuang Autonomous Region Nasopharyngeal Carcinoma January 1, 2017 Phase 2
NCT02863367 Tianjin Medical University Cancer Institute and Hospital Metastatic Pancreatic Cancer August 2016 Phase 2
NCT03048877 Peking Union Medical College Hospital Differentiated Thyroid Cancer December 2016 Phase 3
NCT02942329 The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Gastric Cancer|Hepatocellular Carcinoma October 2016 Phase 1|Phase 2
NCT02691871 Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Jiangsu HengRui Medicine Co., Ltd. Lung Adenocarcinoma February 2016 Phase 1
NCT02525237 Qingdao Municipal Hospital|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer August 2015 Phase 2
NCT02780778 Tianjin Medical University Cancer Institute and Hospital Non-small Cell Lung Cancer May 2016 Phase 2|Phase 3
NCT01270386 Jiangsu HengRui Medicine Co., Ltd.|Sun Yat-sen University Non-Small-Cell Lung Cancer March 2010 Phase 2
NCT02409199 Shanghai Zhongshan Hospital Gastric Carcinoma June 2015 Phase 2|Phase 3
NCT03144843 Sun Yat-sen University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer January 13, 2017 Phase 2
NCT03114085 First Affiliated Hospital of Guangxi Medical University Hepatocellular Carcinoma May 20, 2017 Phase 2
NCT03050411 Peking University Third Hospital Nonsmall Cell Lung Cancer May 2016 Phase 1
NCT02702323 Zhejiang Cancer Hospital|First Affiliated Hospital of Zhejiang University|Second Affiliated Hospital, School of Medicine, Zhejiang University|The Central Hospital of Lishui City|First Affiliated Hospital of Wenzhou Medical Univeristy|Ningbo No.2 Hospital Hepatocellular Carcinoma|Pulmonary Metastasis March 2016 Phase 2|Phase 3
NCT02945852 Zhejiang Cancer Hospital Small Cell Lung Cancer October 2016 Phase 2
NCT03190239 Xinqiao Hospital of Chongqing Advanced Non-squamous Non-small-cell Lung Cancer July 15, 2017 Phase 2
NCT03075462 Jiangsu HengRui Medicine Co., Ltd.|Beijing Cancer Hospital Ovarian Cancer|Triple Negative Breast Cancer March 9, 2017 Phase 1
NCT03116555 China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region Metastatic Gastric Adenocarcinoma April 5, 2017 Phase 2
NCT02768415 Chinese Academy of Medical Sciences Breast Cancer June 2016 Phase 2
NCT02697838 Fujian Cancer Hospital Malignant Neoplasm of Stomach Stage II August 2016
NCT03066557 Jiangsu Cancer Institute & Hospital|Jiangsu HengRui Medicine Co., Ltd. Hepatocellular Carcinoma March 15, 2017
NCT02776527 Tianjin Medical University Cancer Institute and Hospital Gastric Cancer April 2016 Phase 4
NCT02332512 Jiangsu HengRui Medicine Co., Ltd. Carcinoma, Non-Small-Cell Lung January 2015 Phase 3
NCT00970138 Fudan University Gastric Carcinoma June 2009 Phase 2|Phase 3
NCT02764268 Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer June 2016
NCT02529878 The First Affiliated Hospital of Zhejiang Chinese Medical University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer August 2015 Phase 2
NCT01287962 Sun Yat-sen University Non-small Cell Lung Cancer April 2011 Phase 3
NCT03030937 Fujian Cancer Hospital Advanced Gastric Cancer Adenocarcinoma of Esophagogastric Junction February 1, 2017 Phase 2
NCT03213587 Zhejiang Cancer Hospital Nasopharyngeal Carcinoma July 1, 2017 Phase 2
NCT03127319 Affiliated Hospital of Hebei University Non-squamous Non-small Cell Lung Cancer May 2017 Phase 2
NCT03170310 Henan Cancer Hospital|Jiangsu HengRui Medicine Co., Ltd. Advanced Esophagus Cancer February 21, 2017 Phase 2
NCT03100955 Qingdao University Progression Free Survival March 1, 2017 Phase 3
NCT02875457 Third Military Medical University Small Cell Lung Cancer September 2016 Phase 3
NCT03164694 Sun Yat-sen University Lung Cancer May 20, 2017 Phase 2
NCT01512745 Jiangsu HengRui Medicine Co., Ltd.|Fudan University|The 81 Hospital of PLA Advanced or Metastatic Gastric Cancer January 2011 Phase 3
NCT03042611 LSK BioPartners Inc. Gastric Cancer|Gastric Adenocarcinoma February 24, 2017 Phase 3
NCT02596256 Chinese PLA General Hospital Gastric Cancer April 2016 Phase 2
NCT03096184 Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University Head and Neck Squamous Cell Carcinoma May 1, 2017 Phase 2
NCT02980809 First Hospitals affiliated to the China PLA General Hospital Small Cell Lung Cancer March 2017 Phase 2
NCT01531777 Jiangsu HengRui Medicine Co., Ltd.|Fudan University Colorectal Cancer April 2011 Phase 2
NCT03201146 West China Hospital|Jiangsu HengRui Medicine Co., Ltd. Lung Cancer|Non Small Cell Lung Cancer|Combination Chemotherapy|Apatinib June 27, 2017 Phase 1|Phase 2
NCT03192735 Chang-Ming Huang, Prof.|Fujian Medical University Safety and Effectiveness of Apatinib Combined With SOX Neoadjuvant Chemotherapy for Locally Advanced Gastric Cancer July 1, 2017 Phase 2
NCT02510469 Hebei Medical University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer July 2015 Phase 2|Phase 3
NCT03193424 The First Affiliated Hospital of Zhengzhou University Advanced Esophageal Squamous Carcinoma October 2016 Phase 2
NCT02509806 Hebei Medical University|Jiangsu HengRui Medicine Co., Ltd. Gastric Cancer July 2015 Phase 2|Phase 3
NCT02852798 Jiangsu ShengDiYa Medicine Co., Ltd.|Dongguan People's Hospital Nonsquamous Nonsmall Cell Neoplasm of Lung August 2016
NCT02998242 Sichuan Provincial People's Hospital|Chang An Hospital|Hainan Medical College Quality of Life May 2016
NCT02329860 Jiangsu HengRui Medicine Co., Ltd.|NanJing PLA 81 Hospital Carcinoma, Hepatocellular January 13, 2014 Phase 3
NCT03092895 Jiangsu HengRui Medicine Co., Ltd. Advanced Primary Liver Cancer April 27, 2017 Phase 2
NCT03026881 Jiangsu HengRui Medicine Co., Ltd.|The Affiliated Hospital of the Chinese Academy of Military Medical Sciences Recurrent and Metastatic Gastric Cancer January 2017 Phase 1
NCT02704767 The First Affiliated Hospital of Kunming Medical College Lung Cancer June 2016 Phase 2
NCT01497704 LSK BioPartners Inc.|Bukwang Pharmaceutical, Co., Ltd. Cancer Patients With Solid Tumors April 2012 Phase 1|Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.0260 mL 10.1301 mL 20.2601 mL
5 mM 0.4052 mL 2.0260 mL 4.0520 mL
10 mM 0.2026 mL 1.0130 mL 2.0260 mL
Cell Assay
[1]

Apatinib (YN986D1) is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1].

The following human tumor cell lines are used: Ls174t, HCT 116, SGC-7901, HT-29, A549, NCI-H460, Mo7e, A431, BT474 and NIH-3T3. The cells are cultured in RPMI-1640 or DMEM supplemented with 10% FBS at 37°C with 5% carbon dioxide. Primary HUVEC are isolated from segments of normal-term cords by digestion with type I collagenase, and are pooled and cultured in Medium 199 (M199) supplemented with 20% FBS and endothelial cell growth factor. Cells in the exponential growth phase are used in the experiments. The HUVEC are seeded into 96-well plates. After 24 h of incubation, cells are exposed to the test agents (vehicle as control) together with 20 ng/mL VEGF or 20% FBS for another 72 h. After fixation with 10% trichloroacetic acid, the cells are stained with 0.4% sulforhodamine B for 30 min at 37°C and then washed with 1% acetic acid. Tris is added to dissolve the complex, and the optical density is measured at 520 nm[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Apatinib (YN986D1) is diluted in 0.5% (w/v) carboxymethyl cellulose and 5% (w/v) glucose solution (Mice)[1].

Mice[1]
The effects of Apatinib (YN968D1) on tumor growth are tested against various human tumors grown subcutaneously in BALB/cA nude mice. Tumor growth is initiated by subcutaneous inoculation of cells into mice. Tumors are allowed to establish and grow to 100-300 mm3, at which time the mice are randomized into experimental groups. Apatinib is administered once daily by oral gavage for the indicated periods. In combination treatment experiments, mice are administered Apatinib alone by oral gavage; 5-FU, oxaliplatin, docetaxel and doxorubicin alone by intravenous injection; or Apatinib in combination with each cytotoxic drug at the indicated dose and schedule. Tumor volume and bodyweight are monitored every other day or every 3 days, with the means indicated for groups of six (treated) or 12 (vehicle control) animals. Tumor volumes are determined by measuring the largest diameter (a) and its perpendicular (b) according to the formula (a×b2)/2. The evaluation index for inhibition is the relative tumor growth ratio according to the equation: T/C (%)=mean increase of tumor volumes of treated groups⁄mean increase of tumor volumes of control groups×100%. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

493.58

Formula

C₂₅H₂₇N₅O₄S

CAS No.

1218779-75-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.76%

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Apatinib
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