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Rivoceranib Mesylate

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Chemical Structure| 1218779-75-9 同义名 : Apatinib mesylate;YN968D1;Rivoceranib
CAS号 : 1218779-75-9
货号 : A147165
分子式 : C25H27N5O4S
纯度 : 98+%
分子量 : 493.578
MDL号 : MFCD22420814
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

0.5% CMC+water 6 mg/mL suspension

生物活性
靶点

  • VEGFR2

    VEGFR2, IC50:1 nM
描述 Vascular endothelial growth factor (VEGF) regulates angiogenesis and endothelial cell function via binding to three membrane receptor tyrosine kinases: VEGFR‐1, VEGFR‐2, and VEGFR‐3. Apatinib Mesylate is a mesylate form of Apatinib. Apatinib is a selective inhibitor of VEGFR‐2 with an IC50 value of 1 nM. The kinase activities of Ret, c-Kit and c-Src tyrosine kinases could also be potently inhibited by apatinib with IC59 values of 0.013, 0.429 and 0.53 μM, respectively. In human umbilical vein endothelial cells (HUVEC), apatinib decreased VEGF‐stimulated activation of VEGFR‐2/KDR at a dose-dependent manner, and complete inhibition of VEGFR‐2/KDR phosphorylation was observed when 0.1 μM apatinib was applied. Apatinib at 0.01 – 10 μM also suppressed the activation of c‐kit and PDGFRβ in Mo7e and NIH‐3T3 cells. The proliferation of HUVEC induced by 20% FBS was inhibited by apatinib with an IC50 value of 23.4 μM, and the proliferation stimulated by 20 ng/mL VEGF was significantly blocked by apatinib with an IC50 value of 0.17 μM. Apatinib at 1 μM prevented HUVEC from forming the tubes and significantly inhibited FBS-triggered cell migration. Two-week oral administration of apatinib (100 and 200 mg/kg/day, once per day) significantly inhibited tumor growth in immunodeficient mice implanted with human tumor xenografts. In mice implanted with NCI‐H460 tumor, the antitumor effect of apatinib (150 mg/kg/day) alone was enhanced by the combination with docetaxel (12 mg/kg), showing 93% inhibition after two weeks of treatment[4].
作用机制 Apatinib is a small antiangiogenic molecule that specifically binds to the phosphorylation sites of VEGFR-2, inhibiting VEGF binding and subsequent VEGFR-2 autophosphorylation[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.13mL

2.03mL

1.01mL

20.26mL

4.05mL

2.03mL
参考文献

[1]Tian S, Quan H, et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.

[2]Mi YJ, Liang YJ, et al. Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters. Cancer Res. 2010 Oct 15;70(20):7981-91.

[3]Wang Y, Tang Z, et al. A novel long-sustaining system of apatinib for long-term inhibition of the proliferation of hepatocellular carcinoma cells. Onco Targets Ther. 2018 Nov 29;11:8529-8541.

[4]Tian S, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.

[5]Zhang H. Apatinib for molecular targeted therapy in tumor. Drug Des Devel Ther. 2015 Nov 13;9:6075-81.