Apatinib (also known as YN968D1) is an orally bioavailable, small molecule inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR). Apatinib specifically inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. Apatinib also mildly inhibits c-Kit and c-SRC tyrosine kinases. Apatinib (YN968D1) significantly enhanced the cytotoxicity of ABCB1 or ABCG2 substrate drugs in KBv200, MCF-7/adr, and HEK293/ABCB1 cells overexpressing ABCB1 and in S1-M1-80, MCF-7/FLV1000, and HEK293/ABCG2-R2 cells overexpressing ABCG2 (wild-type). Apatinib significantly increased the intracellular accumulation of rhodamine 123 and doxorubicin in the multidrug resistance (MDR) cells. Furthermore, apatinib (YN968D1) significantly increased the ATPase activity of both ABCB1 and ABCG2.
Cell Cycle. 2018;17(10):1235-1244.
Apatinib, a novel tyrosine kinase inhibitor, suppresses tumor growth in cervical cancer and synergizes with Paclitaxel.
Apatinib purchased from AbMole
|Cell lines||HUVEC cells|
|Preparation method||Cell proliferation assays.
The HUVEC were seeded into 96-well plates. After 24 h of incubation, cells were exposed to the test agents (vehicle as control) together with 20 ng⁄ mL VEGF or 20% FBS for another 72 h. After fixation with 10% trichloroacetic acid, the cells were stained with 0.4% sulforhodamine B for 30 min at 37C and then washed with 1% acetic acid. Tris was added to dissolve the complex, and the optical density was measured at 520 nm.
|Concentrations||0.1 and 1μM|
|Incubation time||72 h|
|Animal models||Ls174t, HCT 116, SGC-7901, HT-29, A549, NCI-H460 cells tumour xenograft in BALB/cA nude mice|
|Formulation||0.5% (w ⁄ v) carboxymethyl cellulose and 5% (w ⁄ v) glucose solution|
|Dosages||50, 100, 200 mg/kg once daily for 14, 18 or 21days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
Apatinib (YN968D1) enhances the efficacy of conventional chemotherapeutical drugs in side population cells and ABCB1-overexpressing leukemia cells.
Tong XZ, et al. Biochem Pharmacol. 2012 Mar 1;83(5):586-97. PMID: 22212563.
YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo.
Tian S, et al. Cancer Sci. 2011 Jul;102(7):1374-80. PMID: 21443688.
Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters.
Mi YJ, et al. Cancer Res. 2010 Oct 15;70(20):7981-91. PMID: 20876799.
|Related VEGFR/PDGFR Products|
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BAW2881 (NVP-BAW2881) is a potent and selective VEGFR2 inhibitor with activity to inhibit chronic and acute skin inflammation.
SU 1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM).
Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 7.68 nM.
Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.
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