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. With an IC50 of 1 nM, it inhibits VEGFR2. The Chinese FDA (CFDA) approved apatinib (marketed as Itan® in China) in December 2014 for the treatment of gastric carcinoma in a late stage. In addition to inhibiting cellular phosphorylation of VEGFR-2, c-kit, and PDGFRβ, apatinib potently suppressed the kinase activities of VEGFR-2, c-kit, and c-src. In addition to blocking the budding of rat aortic rings, apatinib effectively inhibited the proliferation, migration, and tube formation of human umbilical vein endothelial cells induced by FBS. Apatinib efficiently and minimally harmed the growth of multiple well-established human tumor xenograft models in vivo, both when used alone and in conjunction with chemotherapeutic drugs.
VEGFR2 (IC50 = 1 nM); RET (IC50 = 13 nM)
Apatinib (YN968D1) exhibited a potent kinase suppression effect on VEGFR-2, c-kit, and c-src, as well as an inhibition of cellular phosphorylation of VEGFR-2, c-kit, and PDGFRβ. With an IC50 of 0.013 μM, 0.429 μM, and 0.53 μM, respectively, YN968D1 suppresses the activities of Ret, c-kit, and c-src. At concentrations up to 10 μM, YN968D1 did not significantly affect EGFR, Her-2, or FGFR1. In addition to blocking the budding of rat aortic ring, YN968D1 efficiently suppressed the proliferation, migration, and tube formation of human umbilical vein endothelial cells stimulated by FBS.
YN968D1 both by itself and in conjunction with chemotherapeutic agents efficiently and minimally harmed the growth of multiple well-established human tumor xenograft models in vivo.
Apatinib, also known as YN968D1, is a newly developed selective inhibitor that can be taken orally and may have antiangiogenic and antineoplastic properties. Apatinib inhibits VEGFR2 by binding to it specifically. Apatinib also has a potent inhibitory effect on Ret, c-kit, and c-src activity, with IC50 values of 0.013 M, 0.429 M, and 0.53 M, respectively. Apatinib prevents PDGFRβ, c-kit, and VEGFR-2 from becoming phosphorylated in cells. Proliferation induced by 20 ng/mL VEGF is significantly inhibited by atainib (IC50 = 0.17μM).
In 96-well plates, the HUVEC were seeded. After incubating for 24 hours, the test agents (vehicle serving as the control) were added to the cells, along with 20 ng ⁄mL VEGF or 20% FBS, and left them for an additional 72 hours. The cells were first fixed with 10% trichloroacetic acid, then stained for 30 minutes at 37°C using 0.4% sulforhodamine B. Afterward, they were cleaned with 1% acetic acid wash. 520 nm optical density was measured after the complex was dissolved with the addition of Tris.
tumor xenograft model (NCI-H460 human lung tumors, HCT 116 human colon tumors, or SGC-7901 human gastric tumors; BALB⁄cA nude mice)
50, 100 and 200 mg/kg
by oral gavage
C, 72.52; H, 5.83; N, 17.62; O, 4.03
|Related CAS #||
811803-05-1; 1218779-75-9 (mesylate); 1218779-89-5 (HCl)
YN968D1; YN-968D1; YN 968D1; Rivoceranib; Apatinib free base
|HS Tariff Code||
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|Solubility (In Vitro)||
|Solubility (In Vivo)||
|Preparing Stock Solutions||1 mg||5 mg||10 mg|
|1 mM||2.5159 mL||12.5796 mL||25.1591 mL|
|5 mM||0.5032 mL||2.5159 mL||5.0318 mL|
|10 mM||0.2516 mL||1.2580 mL||2.5159 mL|
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
In vivo formula preparation method：take μL DMSO mother liquor，join μL Corn oil，mix well and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
Drug: GD regimen
|Ruijin Hospital||August 11, 2019||Phase 2|
|NCT06081595||Not yet recruiting||Drug: Fluzoparib
|Relapsed Ovarian Cancer||Jin Li||October 30, 2023||Phase 2|
|NCT04824352||Recruiting||Drug: apatinib||Effect of Drug
|Peking University People's Hospital||April 1, 2021||Phase 2|
|NCT05235100||Recruiting||Drug: Apatinib Mesylate||Trunk
|Chinese Academy of Medical
|September 1, 2021||Phase 2|
|Gastric Cancer||Peking University||May 11, 2021||Phase 2|
Effects of YN968D1 on various growth factor‐stimulated receptor phosphorylation at the cellular level detected by western blot analysis.Cancer Sci.2011 Jul;102(7):1374-80.
Inhibition of vascular endothelial growth factor (VEGF)‐stimulated HUVEC proliferation, HUVEC tubule formation, HUVEC migration and microvessel outgrowth from rat aortic ring by YN968D1.
Antitumor activity of YN968D1 against human tumor xenografts in nude mice.Cancer Sci.2011 Jul;102(7):1374-80.