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Chemical Structure| 811803-05-1 Chemical Structure| 811803-05-1

Structure of Apatinib
CAS No.: 811803-05-1

Chemical Structure| 811803-05-1

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Apatinib is a selective inhibitor of VEGFR2 with IC50 of 1 nM.

Synonyms: YN968D1; Rivoceranib

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Product Details of Apatinib

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

Safety of Apatinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Apatinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
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:

Species
Animal Model
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 <<

Protocol

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