Structure of Apatinib
CAS No.: 811803-05-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Apatinib is a selective inhibitor of VEGFR2 with IC50 of 1 nM.
Synonyms: YN968D1; Rivoceranib
4.5
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 811803-05-1 |
Formula : | C24H23N5O |
M.W : | 397.47 |
SMILES Code : | O=C(NC1=CC=C(C2(C#N)CCCC2)C=C1)C3=C(NCC4=CC=NC=C4)N=CC=C3 |
Synonyms : |
YN968D1; Rivoceranib
|
MDL No. : | MFCD21648511 |
InChI Key : | WPEWQEMJFLWMLV-UHFFFAOYSA-N |
Pubchem ID : | 11315474 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
In Vitro:
Concentration | Treated Time | Description | References |
Rat vascular smooth muscle cell line A7r5 | 200 nM | 1 hour | Apatinib inhibited PDGF-BB-induced phosphorylation of PDGFR-β, ERK1/2, and JNK. | PMC7520274 |
OCI-Ly19 | 10 µM | 24 h | To investigate the effect of Apatinib in combination with ABT-199 on DLBCL cells, the results showed that the combination significantly inhibited cell proliferation, reduced colony-forming capacity, and induced apoptosis and cell cycle arrest. | PMC9580892 |
OCI-Ly1 | 10 µM | 24 h | To investigate the effect of Apatinib in combination with ABT-199 on DLBCL cells, the results showed that the combination significantly inhibited cell proliferation, reduced colony-forming capacity, and induced apoptosis and cell cycle arrest. | PMC9580892 |
NCI-H345 cells | 50, 100, 150, 200, 250 nM | 24, 48, 72 hours | Apatinib reduced cell proliferation at all concentrations and time points, and cell viability decreased with increasing concentration of apatinib. | PMC8572765 |
KYSE450 | 10, 20, 30, 40, 60 μM | 24, 48, 72 hours | Apatinib significantly inhibited the proliferation of KYSE450 cells and promoted apoptosis. | PMC8980885 |
EC1 | 10, 20, 30, 40, 60 μM | 24, 48, 72 hours | Apatinib significantly inhibited the proliferation of EC1 cells and promoted apoptosis. | PMC8980885 |
A549 | 0, 2, 5, 10 μM | 48 h | Inhibited cell proliferation and promoted apoptosis | PMC8385858 |
H1299 | 0, 2, 5, 10 μM | 48 h | Inhibited cell proliferation and promoted apoptosis | PMC8385858 |
Nalm6 | 55.76 ± 13.19 μM (48 h), 30.34 ± 2.65 μM (72 h) | 48 h, 72 h | Apatinib significantly inhibited the proliferation of Nalm6 cells and induced apoptosis | PMC5831852 |
Reh | 51.53 ± 10.74 μM (48 h), 31.96 ± 3.92 μM (72 h) | 48 h, 72 h | Apatinib significantly inhibited the proliferation of Reh cells and induced apoptosis | PMC5831852 |
Jurkat | 32.43 ± 5.58 μM (48 h), 17.62 ± 5.90 μM (72 h) | 48 h, 72 h | Apatinib significantly inhibited the proliferation of Jurkat cells and induced apoptosis | PMC5831852 |
Molt4 | 39.91 ± 9.88 μM (48 h), 17.65 ± 2.17 μM (72 h) | 48 h, 72 h | Apatinib significantly inhibited the proliferation of Molt4 cells and induced apoptosis | PMC5831852 |
SMMC-7721 | 15 μM | 48 hours | To evaluate the effect of apatinib on the growth of HCC cells, results showed that apatinib suppressed cell viability in a dose-dependent manner. | PMC6836669 |
MHCC-97H | 10 μM | 48 hours | To evaluate the effect of apatinib on the growth of HCC cells, results showed that apatinib suppressed cell viability in a dose-dependent manner. | PMC6836669 |
HCCLM3 | 10 μM | 48 hours | To evaluate the effect of apatinib on the growth of HCC cells, results showed that apatinib suppressed cell viability in a dose-dependent manner. | PMC6836669 |
Hep-3B | 10 μM | 48 hours | To evaluate the effect of apatinib on the growth of HCC cells, results showed that apatinib suppressed cell viability in a dose-dependent manner. | PMC6836669 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
BALB/c Nude mice | Subcutaneous tumor model | Oral | 100 mg/kg | Once daily for 12 days | Inhibited tumor growth | PMC8385858 |
BALB/c Nude mice | osteosarcoma xenograft model | Oral | 50 mg/kg | once daily for 30 days | Apatinib inhibited the growth of osteosarcoma in vivo, and the tumor volume decreased. | PMC5596600 |
BALB/C Nude mice | DLBCL xenograft model | Oral | 100 mg/kg/day | once daily for two weeks | To validate the antitumor efficacy of Apatinib in combination with ABT-199 in DLBCL mouse models, the results showed that the combination therapy significantly reduced tumor volume and weight, and no significant toxicity was observed. | PMC9580892 |
BALB/c Nude mice | SMMC-7721 xenograft model | Oral | 150 mg/kg | Once daily for 4 weeks | To evaluate the effect of apatinib combined with radiotherapy on HCC xenograft tumor model, results showed that the combination treatment significantly suppressed tumor growth. | PMC6836669 |
NSI mice | Acute lymphoblastic leukemia xenograft model | Oral gavage | 100 mg/kg/day | Monday to Friday for 2 consecutive weeks | Apatinib significantly reduced leukemia burden, manifested by a significant decrease in the numbers of human CD45+ cells in the peripheral blood, spleen and bone marrow | PMC5831852 |
Nude mice | mouse xenograft tumour model | Oral gavage | 50 mg/kg | once daily for 37 days | Compared with the control group, tumour sizes in the apatinib-treated mice were significantly reduced on days 34 and 37. | PMC8572765 |
BALB/c Nude mice | EC1 cell xenograft model | Oral | 75 mg/kg | Once daily for 14 days | Apatinib in combination with chemotherapeutic drugs significantly inhibited tumor growth in the EC1 cell xenograft model and promoted tumor cell apoptosis. | PMC8980885 |
C57BL/6 mice | Carotid artery ligation injury model | Intraperitoneal injection | 10 mg/kg/day | Once daily for 14 days | Apatinib significantly reduced the abnormal neointimal area after carotid artery ligation injury. | PMC7520274 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT03709953 | Lung Carcinoma | PHASE2 | UNKNOWN | 2021-04-30 | Zhou Chengzhi, Guangzhou, Guan... More >>gdong, 510120, China Less << |
NCT03376958 | Relapsed and Refractory|Diffus... More >>e Large B Cell Lymphoma Less << | PHASE4 | COMPLETED | 2019-04-30 | Oncology Department of The Fir... More >>st Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, 450052, China Less << |
NCT04152681 | Radiation Injuries | PHASE2 | UNKNOWN | 2025-03-20 | Yamei Tang, Guanzhou, Guangdon... More >>g, 510120, China Less << |
NCT02510469 | Gastric Cancer | PHASE2|PHASE3 | UNKNOWN | 2025-07-18 | Fourth Affiliated Hospital of ... More >>Hebei Medical University, Shijiazhuang, Hebei, 050011, China Less << |
NCT03261791 | Carcinoma, Hepatocellular | PHASE2 | UNKNOWN | 2020-04-20 | Zhongshan Hospital, Shanghai, ... More >>Shanghai, 20032, China Less << |
NCT02727309 | Hepatocellular Carcinoma | PHASE1|PHASE2 | UNKNOWN | 2025-03-19 | Department of Interventional T... More >>herapy, Beijing, Beijing, 100142, China Less << |
NCT03334591 | Two Different Treatment Method... More >>s Less << | PHASE2 | UNKNOWN | 2019-12-01 | Anhui Provincial Cancer Hospit... More >>al, Hefei, Anhui, 230000, China Less << |
NCT02878057 | Breast Cancer | PHASE2 | COMPLETED | 2020-09-02 | - |
NCT03170310 | Advanced Esophagus Cancer | PHASE2 | UNKNOWN | 2019-09-21 | Henan Cancer Hospital/The affi... More >>liated Cancer Hospital of ZhengZhou university, ZhengZhou, Henan, 450008, China Less << |
NCT03547375 | Ovarian Cancer | PHASE2 | UNKNOWN | 2020-06-01 | - |
NCT02544737 | Esophageal Cancer|Metastatic E... More >>sophageal Cancer|Apatinib Less << | PHASE2 | UNKNOWN | 2025-12-17 | Hangzhou Cancer Hospital, Hang... More >>zhou, Zhejiang, 310000, China Less << |
NCT02989259 | Head and Neck Neoplasms | PHASE2 | UNKNOWN | 2025-12-21 | Cancer Hospital, Chinese Acade... More >>my of Medical Sciences (CAMS) & Peking Union Medical College (PUMC), Beijing, Beijing, 100021, China Less << |
NCT03650738 | Systematic Review of the pCR R... More >>ate of Apatinib Combined With Albumin Paclitaxel and Carboplatin Regimen for Neoadjuvant Therapy of Triple-negative Breast Cancer Less << | PHASE2 | UNKNOWN | 2019-12-31 | Jiangsu Provincial Hospital, N... More >>anjing, Jiangsu, 210000, China Less << |
NCT03427242 | Biliary Tract Neoplasms | PHASE2 | UNKNOWN | 2022-10-31 | Fudan University Shanghai Canc... More >>er Center, Shanghai, Shanghai, 200032, China Less << |
NCT03384511 | Malignancies|Stomach Cancer|No... More >>n-small Cell Lung Cancer|Esophageal Cancer|Breast Cancer|Ovary Cancer|Cervical Cancer Less << | PHASE4 | COMPLETED | 2018-01-28 | Jinan, Shandong, 250117, China |
NCT03121846 | Soft Tissue Sarcoma, Adult, St... More >>age II Less << | PHASE2 | UNKNOWN | 2019-05-01 | Tianjin Medical University Can... More >>cer Hospital & Institute, Tianjin, Tianjin, 300060, China Less << |
NCT03020979 | Malignant Ascites|Apatinib | PHASE2 | UNKNOWN | 2025-12-19 | Qiong Wu, Bengbu, Anhui, China |
NCT03654612 | Head and Neck Cancer | PHASE1|PHASE2 | UNKNOWN | 2021-09-01 | the Second Xiangya Hospital, C... More >>hangsha, Hunan, 410011, China Less << |
NCT03271073 | Gastric Cancer | PHASE2 | UNKNOWN | 2019-01-31 | Beijing Friendship Hospital, B... More >>eijing, Beijing, 100050, China Less << |
NCT03199677 | Refractory Cancer | PHASE2 | UNKNOWN | 2018-06-30 | Cancer Hospital, Chinese Acade... More >>my of Medical Sciences, Beijing, Beijing, 100021, China Less << |
NCT04253873 | High-grade Gliomas | PHASE2 | UNKNOWN | 2022-12-30 | Henan Cancer Hospital, Zhengzh... More >>ou, Henan, 450008, China Less << |
NCT03104283 | Gastric Cancer | PHASE2 | COMPLETED | 2020-06-02 | Affiliated Hospital of Qinghai... More >> University, Xining, Qinghai, 810000, China|People's Hospital of Qinghai Province, Xining, Qinghai, 810000, China|Qinghai Red Cross Hospital, Xining, Qinghai, 810000, China|the Fifth People's Hospital of Qinghai Province, Xining, Qinghai, 810000, China|Yangquan No.1 People's Hospital, Yangquan, Shanxi, 045000, China Less << |
NCT04180007 | Thyroid|Metastasis|Apatinib | PHASE2 | UNKNOWN | 2020-05-30 | Nanjing First Hospital, Nanjin... More >>g, Jingsu, 210006, China Less << |
NCT03758677 | Non Small Cell Lung Cancer | PHASE2 | UNKNOWN | 2021-11-20 | The First Hospital of Jilin Un... More >>iversity, Changchun, Jilin, 130021, China Less << |
NCT03243838 | Triple-Negative Breast Cancer | PHASE2 | COMPLETED | 2021-12-31 | Guangdong general hospital, Gu... More >>angzhou, Guangdong, 510080, China|Guangdong General Hospital, Guangzhou, China Less << |
NCT03403452 | Colorectal Cancer | PHASE2 | UNKNOWN | 2019-12-31 | Department of General Surgery,... More >> Zhongshan Hospital, Fudan University, Shanghai, 200032, China Less << |
NCT03521219 | Intrahepatic Cholangiocarcinom... More >>a Less << | PHASE2 | UNKNOWN | 2025-11-19 | The First Affiliated Hospital ... More >>of Zhengzhou University, Zhengzhou, Henan, 450000, China Less << |
NCT05029453 | Gastric Cancer|Randomized Cont... More >>rolled Study Less << | PHASE4 | UNKNOWN | 2023-03-03 | Cancer Center, Union Hospital,... More >> Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, 430022, China Less << |
NCT03104335 | Soft Tissue Sarcoma Adult|Adva... More >>nced Cancer Less << | PHASE2 | WITHDRAWN | 2020-03-01 | Peking University People's Hos... More >>pital, Beijing, Beijing, 100044, China|Peking University Shougang Hospital, Beijing, Beijing, 100144, China|Peking University International Hospital, Beijing, Beijing, 102206, China Less << |
NCT03251443 | Intrahepatic Cholangiocarcinom... More >>a|Second-line Treatment Less << | PHASE2 | COMPLETED | 2019-05-08 | Peking Union Medical College H... More >>ospital, Beijing, Beijing, 100730, China Less << |
NCT03193424 | Advanced Esophageal Squamous C... More >>arcinoma Less << | PHASE2 | UNKNOWN | 2019-12-30 | FirstAHZhengzhouU, Zhengzhou, ... More >>Henan, 450000, China Less << |
NCT03587129 | Ovarian Cancer | PHASE2 | TERMINATED | 2020-06-14 | The First Affiliated Hospital ... More >>of Harbin Medical University, Harbin, Heilongjiang, 150001, China Less << |
NCT01176669 | Metastatic Breast Cancer | PHASE2 | COMPLETED | 2025-09-14 | Fudan University Cancer Hospit... More >>al, Shanghai, Shanghai, 200032, China Less << |
NCT03163381 | Osteosarcoma, Advanced | PHASE2 | UNKNOWN | 2019-04-11 | Henan cancer hospital, Zhengzh... More >>ou, Henan, 450000, China Less << |
NCT01653561 | Breast Neoplasms | PHASE2 | COMPLETED | 2025-10-12 | Fudan University Cancer Hospit... More >>al, Shanghai, Shanghai, 200032, China|Fudan University Cancer Hospital, Shanghai, 200032, China Less << |
NCT03383237 | Malignant Melanoma | PHASE2 | UNKNOWN | 2025-11-19 | Henan Cancer Hospital, Zhengzh... More >>ou, Henan, 450008, China Less << |
NCT04216550 | Recurrent Glioma | RECRUITING | 2025-06-01 | Department of Neurosurgery, Fi... More >>rst Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, 450052, China Less << | |
NCT03542422 | Advanced Esophagus Cancer | PHASE2 | UNKNOWN | 2025-05-19 | Affiliated Hospital of North S... More >>ichuan Medical College, Nanchong, Sichuan, 600000, China Less << |
NCT01192971 | Advanced Hepatocellular Carcin... More >>oma Less << | PHASE2 | COMPLETED | 2025-07-13 | Nanjing Millitary Eighty-one H... More >>osiptal, Nanjing, Jiangsu, 210002, China Less << |
NCT03046979 | Hepatocellular Carcinoma | PHASE2 | UNKNOWN | 2025-12-18 | Tianjin Medical University Can... More >>cer Institute and Hospital, Tianjin, 300060, China Less << |
NCT03274011 | Esophageal Neoplasms | PHASE2 | COMPLETED | 2019-06-26 | Shanghai Yangpu District East ... More >>Hospital, Shanghai, Shanghai, 200433, China Less << |
NCT02726854 | Pancreatic Neoplasms | PHASE2 | UNKNOWN | 2025-12-17 | First affiliate hospital of Xi... More >>'an Jiaotong University, Xi'an, Shaanxi, 710061, China Less << |
NCT02774200 | Metastatic Renal Cell Carcinom... More >>a Less << | PHASE2 | UNKNOWN | 2025-06-17 | - |
NCT03285906 | Esophagus Cancer, Stage III|Es... More >>ophageal Gastric Cardia Type Metaplasia|Esophagus Cancer, Stage IV Less << | PHASE2|PHASE3 | UNKNOWN | 2025-12-19 | Tianjin Medical University Can... More >>cer Institute and Hospital, Tianjin, Tianjin, 300060, China Less << |
NCT03086785 | Breast Cancer Metastatic | PHASE2 | UNKNOWN | 2025-05-19 | Fourth Hospital of Hebei Medic... More >>al University, ShiJiazhuang, Hebei, 050019, China Less << |
NCT03599778 | Gastric Carcinoma | PHASE1|PHASE2 | UNKNOWN | 2025-01-30 | Anhui Provincial Cancer Hospit... More >>al, Hefei, Anhui, 230000, China Less << |
NCT03634059 | NSCLC | UNKNOWN | 2020-08-15 | Junfeng Liu, Shijiazhuang, Heb... More >>ei, 050000, China Less << | |
NCT03029013 | Cervical Cancer | UNKNOWN | 2025-12-20 | Daping Hospital, Third Militar... More >>y Medical University, Chongqing, Chongqing, 400042, China Less << | |
NCT02764268 | Gastric Cancer | COMPLETED | 2019-04-15 | Shanghai 6th People's Hospital... More >>, Shanghai, Shanghai, 200233, China Less << | |
NCT03144856 | Biliary Tract Cancer | PHASE2 | UNKNOWN | 2019-03-01 | Foshan people's Hospital, Fosh... More >>an, Guangdong, China|Cancer center of Sun Yat-sen University, Guangzhou, Guangdong, 510060, China Less << |
NCT03129698 | Apatinib in Maintenance Treatm... More >>ent Less << | PHASE2 | UNKNOWN | 2020-03-01 | Junling Li, Beijing, Beijing, ... More >>100021, China Less << |
NCT03546855 | Cervical Cancer | PHASE2 | UNKNOWN | 2020-06-01 | - |
NCT03376737 | Lung Adenocarcinoma | PHASE2 | UNKNOWN | 2025-06-19 | Henan Cancer Hospital, Zhengzh... More >>ou, Henan, 450008, China Less << |
NCT03390062 | Glioma | PHASE2 | UNKNOWN | 2020-08-01 | - |
NCT03180476 | Nasopharyngeal Neoplasms | PHASE2 | COMPLETED | 2020-04-01 | Sichuan Cancer Hospital, Chend... More >>u, Sichuan, 600000, China Less << |
NCT03801200 | NSCLC | PHASE2 | UNKNOWN | 2023-09-10 | Hubei Cancer hospital, Wuhan, ... More >>Hubei, 430079, China Less << |
NCT03725423 | Lung Squamous Cell Carcinoma | PHASE4 | UNKNOWN | 2025-06-19 | - |
NCT02509806 | Gastric Cancer | PHASE2|PHASE3 | UNKNOWN | 2025-12-17 | Fourth Affiliated Hospital of ... More >>Hebei Medical University, Shijiazhuang, Hebei, 050011, China Less << |
NCT03213587 | Nasopharyngeal Carcinoma | PHASE2 | UNKNOWN | 2025-07-20 | Xiaozhong Chen, Hangzhou, Zhej... More >>iang, 310022, China Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.16mL 5.03mL 2.52mL |