Catalog No.S2221 Synonyms: YN968D1
Molecular Weight(MW): 493.58
Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.|
|Features||Good anti-tumor effects for gastric and colorectal cancer compared with sorafenib and sunitinib.|
Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. Apatinib can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring.  Apatinib reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatinib significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [125I]iodoarylazidoprazosin in a concentration-dependent manner. 
|In vivo||Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner.  Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model.  Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. |
|In vitro||DMSO||22 mg/mL (44.57 mM)|
|In vivo||0.5% CMC||6 mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02836171||Recruiting||Neoplasms||Jiangsu HengRui Medicine Co., Ltd.||July 2016||Phase 1|
|NCT02844881||Not yet recruiting||Advanced Solid Tumors|Excluding T Cell Lymphoma||The First Peoples Hospital of Lianyungang|HengRui YuanZheng Bio-Technology Co.,Ltd.||July 2016||Phase 1|Phase 2|
|NCT02848794||Not yet recruiting||High-grade Glioma||The First Peoples 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||July 2016||Phase 1|Phase 2|
|NCT02824458||Recruiting||EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors||Sun Yat-sen University||June 2016||Phase 3|
|NCT02829385||Recruiting||Colorectal Neoplasms||Shoucheng Ma|LanZhou University||June 2016||Phase 2|
|NCT02775370||Not yet recruiting||Adenoid Cystic Carcinoma||Shanghai Ninth Peoples Hospital Affiliated to Shanghai Jiao Tong University||June 2016||Phase 2|
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