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Formula | C24H23N5O |
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Molecular Weight | 397.47 | CAS No. | 811803-05-1 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (251.59 mM) | ||||||||
Water | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis. | ||||
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Targets |
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In vitro | Apatinib (YN968D1) potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. YN968D1 suppress the activities of Ret, c-kit and c-src with an IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. YN968D1 had no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM. YN968D1 effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring[1]. | ||||
In vivo | In vivo, YN968D1 alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity[1]. |
Cell Assay: |
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Animal Study: |
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Pharmacogenomic profiling of intra-tumor heterogeneity using a large organoid biobank of liver cancer [ Cancer Cell, 2024, 42(4):535-551.e8] | PubMed: 38593780 |
Targeting the VEGFR2 signaling pathway for angiogenesis and fibrosis regulation in neovascular age-related macular degeneration [ Sci Rep, 2024, 14(1):25682] | PubMed: 39465270 |
Apatinib weakens proliferation, migration, invasion, and angiogenesis of thyroid cancer cells through downregulating pyruvate kinase M2 [ Sci Rep, 2024, 14(1):879] | PubMed: 38195651 |
N4-Acetylcytidine Drives Glycolysis Addiction in Gastric Cancer via NAT10/SEPT9/HIF-1α Positive Feedback Loop [ Adv Sci (Weinh), 2023, 10(23):e2300898] | PubMed: 37328448 |
HER4 and EGFR activate cell signaling in NRG1 fusion-driven cancers: implications for HER2/HER3-specific vs. pan-HER targeting strategies [ J Thorac Oncol, 2023, S1556-0864(23)00802-X] | PubMed: 37678511 |
Integrative analysis of multi-omics data reveals inhibition of RB1 signaling promotes apatinib resistance of hepatocellular carcinoma [ Int J Biol Sci, 2023, 19(14):4511-4524] | PubMed: 37781033 |
Dihydroartemisinin Potentiates VEGFR-TKIs Antitumorigenic Effect on Osteosarcoma by Regulating Loxl2/VEGFA Expression and Lipid Metabolism Pathway [ J Cancer, 2023, 14(5):809-820] | PubMed: 37056396 |
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599] | PubMed: 37797618 |
The interactions between integrin α5β1 of liver cancer cells and fibronectin of fibroblasts promote tumor growth and angiogenesis [ Int J Biol Sci, 2022, 18(13):5019-5037] | PubMed: 35982891 |
Apatinib enhances chemosensitivity of ABT-199 in diffuse large B-cell lymphoma [ Mol Oncol, 2022, 16(20):3735-3753] | PubMed: 36053810 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.