Catalog No.S5248 Synonyms: YN968D1
Molecular Weight(MW): 397.47
Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.
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|Description||Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.|
Apatinib (YN968D1) potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. YN968D1 suppress the activities of Ret, c-kit and c-src with an IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. YN968D1 had no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM. YN968D1 effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring.
|In vivo||In vivo, YN968D1 alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity.|
|In vitro||DMSO||79 mg/mL (198.75 mM)|
|Ethanol||10 mg/mL (25.15 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03743428||Recruiting||Drug: Apatinib Mesylate Tablets|Drug: Bevacizumab Injection||Colorectal Neoplasms||Shenzhen People''s Hospital||October 22 2019||Not Applicable|
|NCT03878472||Not yet recruiting||Drug: SHR1210|Drug: apatinib|Drug: S1||Gastric Cancer||Qilu Hospital of Shandong University||April 1 2019||Phase 2|
|NCT03816553||Recruiting||Drug: SHR-1210|Drug: Apatinib||Recurrent Cervical Carcinoma|Metastatic Cervical Cancer||Sun Yat-sen University||January 19 2019||Phase 2|
|NCT03764293||Not yet recruiting||Drug: SHR-1210|Drug: Apatinib|Drug: Sorafenib||Locally Advanced or Metastatic and Unresectable HCC||Jiangsu HengRui Medicine Co. Ltd.||January 2019||Phase 3|
|NCT03407976||Recruiting||Drug: Apatinib|Drug: Pembrolizumab||Advanced Malignancies|Urothelial Carcinoma|MSI-H or dMMR Solid Tumors|Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma||University of Utah|LSK BioPartners Inc.||June 19 2018||Phase 1|Phase 2|
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