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Apatinib

Cat. No. M1956
Apatinib Structure
Synonym:

YN968D1

Size Price Availability Quantity
10mg USD 140 In stock
50mg USD 320 In stock
100mg USD 535 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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 Experiment
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
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 493.58
Formula C25H27N5O4S
CAS Number 811803-05-1
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Apatinib, YN968D1 supplier, VEGFR/PDGFR, inhibitors

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