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|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03042611||Not yet recruiting||Gastric Cancer|Gastric Adenocarcinoma||LSK BioPartners Inc.||February 7, 2017||Phase 3|
|NCT02980809||Not yet recruiting||Small Cell Lung Cancer||First Hospitals affiliated to the China PLA General Hospital||March 2017||Phase 2|
|NCT03029013||Recruiting||Cervical Cancer||Third Military Medical University||January 2017||--|
|NCT03020979||Not yet recruiting||Malignant Ascites|Apatinib||First Affiliated Hospital Bengbu Medical College||January 2017||Phase 2|
|NCT03026881||Not yet recruiting||Recurrent and Metastatic Gastric Cancer||Jiangsu HengRui Medicine Co., Ltd.|Affiliated Hospital of Academy of Military Medical Sciences,China||January 2017||Phase 1|
|NCT02995187||Not yet recruiting||Small Cell Lung Cancer||Chinese Academy of Medical Sciences||December 2016||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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