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    Apatinib (Rivoceranib, YN968D1)
    Apatinib (Rivoceranib, YN968D1)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0503
    CAS #: 811803-05-1 (free base)Purity ≥98%

    Description: Apatinib (formerly known as Rivoceranib, YN-968D1) is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway with potential antiangiogenic and antineoplastic activities. It inhibits VEGFR2 with an IC50 of 1 nM. Apatinib (Aitan®, trade name in China) was approved by the Chinese FDA (CFDA) in December 2014 foe the treatment of late-stage gastric carcinoma. Apatinib potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib 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, Apatinib alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity. 

    References: Cancer Sci. 2011;102(7):1374-80; Cancer Res. 2010;70(20):7981-91; Biochem Pharmacol. 2012;83(5):586-97. 

    Related CAS: 811803-05-1 (free base); 1218779-75-9 (mesylate)

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    Molecular Weight (MW)397.47
    FormulaC24H23N5O
    CAS No. 811803-05-1 (free base)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 22 mg/mL (44.57 mM) 
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)0.5% CMC: 6mg/mL
    SynonymsYN968D1;YN-968D1; YN 968D1; Rivoceranib; Apatinib free base; 

    Chemical Name: N-(4-(1-cyanocyclopentyl)phenyl)-2-((4-methylpyridin-3-yl)amino)nicotinamide

    InChi Key: MGZNERAVOCFMCU-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H23N5O/c1-17-10-14-26-15-21(17)29-22-20(5-4-13-27-22)23(30)28-19-8-6-18(7-9-19)24(16-25)11-2-3-12-24/h4-10,13-15H,2-3,11-12H2,1H3,(H,27,29)(H,28,30)

    SMILES Code: O=C(NC1=CC=C(C2(C#N)CCCC2)C=C1)C3=C(NC4=C(C)C=CN=C4)N=CC=C3



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    In Vitro

    In vitro activity:  Apatinib is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway with IC50 of 1 nM for VEGFR2. It has potential antiangiogenic and antineoplastic activities. Apatinib potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. A phase I study of Apatinib has shown encouraging antitumor activity and a manageable toxicity profile. These findings suggest that Apatinib has promise as an antitumor drug and might have clinical benefits. 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.


    Kinase Assay:  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).


    Cell Assay: In HUVEC, Apatinib decreases VEGF-stimulated phosphorylation of VEGFR-2 KDR in a concentration-dependent manner. It also completely inhibits VEGFR-2 activation at a concentration of 0.1 μM. Furthermore, Apatinib abrogates the phosphorylation of c-kit and PDGFRb in Mo7e and NIH-3T3 cells stimulated with the relevant ligand, respectively, in a concentration-dependent manner. In addition, Apatinib inhibits proliferation, migration and tube formation of HUVEC in vitro and blocking of rat aortic ring budding.

    In VivoIn vivo, Apatinib alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity. 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. 
    Animal modelNude mice human tumor xenografts
    Formulation & DosageFormulated in 0.5% (w/v) carboxymethyl cellulose; 50, 100, 200 mg/kg; oral gavage
    ReferencesCancer Sci. 2011 Jul;102(7):1374-80; Cancer Res. 2010 Oct 15;70(20):7981-91; Biochem Pharmacol. 2012 Mar 1;83(5):586-97. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Apatinib

    Effects of YN968D1 on various growth factor‐stimulated receptor phosphorylation at the cellular level detected by western blot analysis.  2011 Jul;102(7):1374-80.


    Apatinib

    Inhibition of vascular endothelial growth factor (VEGF)‐stimulated HUVEC proliferation, HUVEC tubule formation, HUVEC migration and microvessel outgrowth from rat aortic ring by YN968D1.

    Apatinib

    Antitumor activity of YN968D1 against human tumor xenografts in nude mice.   2011 Jul;102(7):1374-80.


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