Apatinib Mesylate (Synonyms: YN968D1) |
Catalog No.GC14292
One-Click Copy Product Info
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Apatinib Mesylate blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 811803-05-1
Sample solution is provided at 25 µL, 10mM.
Apatinib Mesylate is a potent, orally bioavailable, ATP-competitive VEGFR-2 tyrosine kinase inhibitor with a cell-free IC₅₀ of 1nM[1]. Apatinib Mesylate suppresses VEGFR-2 phosphorylation and downstream PLCγ1/ERK1/2, PI3K/AKT, and STAT3 signaling, thereby limiting cell proliferation, survival, migration, and angiogenesis[1][2][4]. Apatinib Mesylate is used in research on tumor angiogenesis, solid-tumor growth and migration, leukemia biology, autophagy, and ABC-transporter-mediated multidrug resistance[2][3][4][5][6][7].
In vitro, Apatinib Mesylate inhibited VEGF-stimulated human umbilical vein endothelial cell proliferation over 72h with an IC₅₀ of 0.17μM, whereas the IC₅₀ against 20% fetal bovine serum-stimulated proliferation was 23.4μM[1]. In SGC-7901 and BGC-823 human gastric cancer cells, Apatinib Mesylate (100, 500, and 1000nM; 24h) reduced proliferation and VEGF secretion; Apatinib Mesylate (500nM overnight; VEGF stimulation for 30min) reduced phosphorylation of VEGFR-2, PLCγ1, and ERK1/2, while MGC-803 cells with low pathway activity showed no significant proliferation response[2]. In KHOS and MG63 human osteosarcoma cells, Apatinib Mesylate (10μM; 48h) increased apoptosis and autophagic markers, induced G0/G1 arrest, and reduced STAT3 and BCL-2 signaling[3]. In Jurkat and Nalm6 human acute lymphoblastic leukemia cells, Apatinib Mesylate (0, 10, 20, and 40μM; 48h) dose-dependently reduced VEGFR-2, ERK, AKT, and STAT3 pathway activation[4]. In human malignant peritoneal mesothelioma cells, Apatinib Mesylate (0, 12.5, 25, 50, and 100μM; 24, 48, and 72h) inhibited proliferation in concentration- and time-dependent manners, with IC₅₀ values of 46.34μM, 45.14μM, and 28.73μM at 24, 48, and 72h, respectively[5].
In vivo, female nude mice bearing CNE-2 human nasopharyngeal carcinoma xenografts received Apatinib Mesylate (200mg/kg/day; intragastric gavage once daily for 7 days), which reduced the VEGFR-2-positive tumor-cell proportion from 92.83% to 54.50%, decreased CD31-defined microvessel density from 8.67 to 5.00, and inhibited tumor growth[6]. NODscid-IL2Rg⁻/⁻ mice bearing Nalm6 human acute lymphoblastic leukemia xenografts received Apatinib Mesylate (100mg/kg/day; oral gavage once daily from Monday to Friday for 2 weeks), which reduced human CD45-positive leukemia cells in peripheral blood, bone marrow, and spleen and decreased spleen weight[4]. In ABCB1-overexpressing KBv200 human cancer nude mouse xenograft model, Apatinib Mesylate (70mg/kg; oral administration every 3 days for four doses; 1h before paclitaxel) enhanced the antitumor activity of paclitaxel and produced 52.7% tumor-growth inhibition without apparent body-weight loss[7].
References:
[1] 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;102(7):1374-1380. doi:10.1111/j.1349-7006.2011.01939.x.
[2] Lin Y, Zhai E, Liao B, Xu L, Zhang X, Peng S, et al. Autocrine VEGF signaling promotes cell proliferation through a PLC-dependent pathway and modulates Apatinib treatment efficacy in gastric cancer. Oncotarget. 2017;8(7):11990-12002. doi:10.18632/oncotarget.14467.
[3] Liu K, Ren T, Huang Y, Sun K, Bao X, Wang S, Zheng B, Guo W. Apatinib promotes autophagy and apoptosis through VEGFR2/STAT3/BCL-2 signaling in osteosarcoma. Cell Death Dis. 2017;8:e3015. doi:10.1038/cddis.2017.422.
[4] Deng M, Zha J, Jiang Z, Jia X, Shi Y, Li P, et al. Apatinib exhibits anti-leukemia activity in preclinical models of acute lymphoblastic leukemia. J Transl Med. 2018;16:47. doi:10.1186/s12967-018-1421-y.
[5] Yang ZR, Chen ZG, Du XM, Li Y. Apatinib Mesylate Inhibits the Proliferation and Metastasis of Epithelioid Malignant Peritoneal Mesothelioma In Vitro and In Vivo. Front Oncol. 2020;10:585079. doi:10.3389/fonc.2020.585079.
[6] Peng QX, Han YW, Zhang YL, Hu J, Fan J, Fu SZ, Xu S, Wan Q. Apatinib inhibits VEGFR-2 and angiogenesis in an in vivo murine model of nasopharyngeal carcinoma. Oncotarget. 2017;8:52813-52822. doi:10.18632/oncotarget.17264.
[7] Mi YJ, Liang YJ, Huang HB, Zhao HY, Wu CP, Wang F, et al. Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters. Cancer Res. 2010;70(20):7981-7991. doi:10.1158/0008-5472.CAN-10-0111.
| Cell experiment [1]: | |
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Cell lines |
SGC-7901, BGC-823, and MGC-803 human gastric cancer cells |
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Preparation Method |
Cells were seeded in 96-well plates at 2×10³ cells/well and treated with Apatinib Mesylate. Cell viability was measured by CCK-8 assay, and VEGF in culture medium was measured by ELISA. For pathway analysis, SGC-7901 and BGC-823 cells were treated with Apatinib Mesylate overnight and then stimulated with recombinant human VEGF before p-VEGFR-2, p-PLCγ1, and p-ERK1/2 were examined by western blotting. |
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Reaction Conditions |
100, 500, and 1000nM for 24h; 500nM overnight followed by VEGF stimulation for 30min |
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Applications |
Apatinib Mesylate significantly inhibited proliferation and VEGF secretion in SGC-7901 and BGC-823 cells with high VEGFR-2 pathway activity, but not in MGC-803 cells with low pathway activity. Apatinib Mesylate at 500nM reduced VEGF-induced phosphorylation of VEGFR-2, PLCγ1, and ERK1/2 to below baseline levels. |
| Animal experiment [2]: | |
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Animal models |
Subcutaneous CNE-2 human nasopharyngeal carcinoma xenografts in 4-week-old female nude mice |
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Preparation Method |
When mean tumor volume reached 100mm³, mice were randomized. The Apatinib Mesylate group received daily intragastric gavage, and the vehicle group received saline by the same route. Tumor volume and body weight were recorded every 2 days. At the end of treatment, tumors were weighed and analyzed by VEGFR-2 and CD31 immunohistochemistry, TUNEL, and ¹⁸F-FDG PET/CT. |
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Dosage form |
200mg/kg/day; intragastric gavage once daily for 7 days |
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Applications |
Apatinib Mesylate reduced the proportion of VEGFR-2-positive tumor cells from 92.83% to 54.50% and decreased CD31-defined microvessel density from 8.67 to 5.00. Tumor metabolic activity and CNE-2 xenograft growth were also reduced. |
References: [1] Lin Y, Zhai E, Liao B, Xu L, Zhang X, Peng S, et al. Autocrine VEGF signaling promotes cell proliferation through a PLC-dependent pathway and modulates Apatinib treatment efficacy in gastric cancer. Oncotarget. 2017;8(7):11990-12002. doi:10.18632/oncotarget.14467. [2] Peng QX, Han YW, Zhang YL, Hu J, Fan J, Fu SZ, Xu S, Wan Q. Apatinib inhibits VEGFR-2 and angiogenesis in an in vivo murine model of nasopharyngeal carcinoma. Oncotarget. 2017;8:52813-52822. doi:10.18632/oncotarget.17264. | |
| Cas No. | 811803-05-1 | SDF | |
| Synonyms | YN968D1 | ||
| Chemical Name | N-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide;methanesulfonic acid | ||
| Canonical SMILES | CS(=O)(=O)O.C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4 | ||
| Formula | C25H27N5O4S | M.Wt | 493.58 |
| Solubility | ≥ 49.4mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.026 mL | 10.1301 mL | 20.2601 mL |
| 5 mM | 405.2 μL | 2.026 mL | 4.052 mL |
| 10 mM | 202.6 μL | 1.013 mL | 2.026 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Related Biological Data
VEGFA derived from hypoxic PMCs facilitates GC cell adhesion and migration via VEGFR1. a The effect of exogenous VEGFA on cell migration was observed in the presence of Apatinib or Bevacizumab. Representative photographs of migratory cells are shown. Scale bar represents 100 μm.
Apatinib were obtained from GlpBio.
J Exp Clin Canc Res 39.1 (2020): 1-14. PMID: 33081836 IF: 11.163 -
Related Biological Data
Targeting SMYD2 synergistically increases the antiangiogenic activity of apatinib in CRC.IHC staining revealed that both BAY-598 and apatinib treatment reduced CD31 levels, but more satisfactory effects were achieved when the two treatments were combined.
Then, we treated CRC cells with DMSO, BAY-598, apatinib (10 μM), or BAY-598 (10 μM) combined with apatinib(GLPBIO) for 48 h, and prepared TCM according to the standard method.
Angiogenesis (2022): 1-18. PMID: 35503397 IF: 9.5957 -
Related Biological Data
Art-M improves the antitumor effect of apatinib in GC both in vivo and in vitro. (A) Total number of viable cells was counted after treatment of MGC803 and AGS cells with different concentrations of apatinib for 96 h.
Male nude mice carrying GC xenografts were randomly divided into four groups and given Art-M (2 mg/kg; i.p.; once daily), apatinib(GlpBio) (50 mg/kg; p.o.; once daily), or both for 24 days.
Chem-Biol Interact (2023): 110618. PMID: 37394161 IF: 5.1
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