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.
J Cancer Res Clin Oncol. 2022 Aug 11.
The crosstalk between lung cancer cells and platelets promotes tumor angiogenesis in vivo and in vitro
Apatinib mesylate purchased from AbMole
Phytomedicine. 2022 Jun;100:154068.
Geniposide alleviates VEGF-induced angiogenesis by inhibiting VEGFR2/PKC/ERK1/2-mediated SphK1 translocation
Apatinib mesylate purchased from AbMole
Cell Cycle. 2018;17(10):1235-1244.
Apatinib, a novel tyrosine kinase inhibitor, suppresses tumor growth in cervical cancer and synergizes with Paclitaxel.
Apatinib mesylate purchased from AbMole
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Source | Cell Cycle (2018 Jul). Figure 4. Apatinib (Abmole Bioscience) |
| Method | cellular proliferation assay | |
| Cell Lines | SiHa cells | |
| Concentrations | 20 μM | |
| Incubation Time | 24 hour | |
| Results | In addition, Gene Ontology analysis showed that the genes involved in mitotic cell cycle (both G1/S transition and G2/M transition), cell division, DNA repair, and cell proliferation were under the precise regulation of Apatinib |
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Source | Cell Cycle (2018 Jul). Figure 3. Apatinib (Abmole Bioscience) |
| Method | cellular proliferation assay | |
| Cell Lines | SiHa and Hcc94 cells | |
| Concentrations | 10 μM and 20 μM | |
| Incubation Time | 24 hour | |
| Results | Then we detected the effects of Apatinib on cellular mitochondrial membrane potential (an apoptotic marker). |
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Source | Cell Cycle (2018 Jul). Figure 2. Apatinib (Abmole Bioscience) |
| Method | cellular proliferation assay | |
| Cell Lines | C33A and HeLa cells | |
| Concentrations | 10 μM and 20 μM | |
| Incubation Time | 24 hour | |
| Results | Further, the 24-hour treatment of Apatinib induced significant G1-phase arrest in a dose-dependent manner in both SiHa and Hcc94 cells |
| 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 |
| Molecular Weight | 493.58 |
| Formula | C25H27N5O4S |
| CAS Number | 1218779-75-9 |
| Solubility (25°C) | DMSO 22 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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Jolkinolide A is a diterpenoid, which exhibits anti-tumor activity, by affecting on angiogenesis of tumor tissues. Jolkinolide A significantly inhibits the Akt-STAT3-mTOR signaling pathway and reduces the expression of VEGF in A549 cells. |
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