Apatinib

Catalog No.S5248 Batch:S524806

Technical Data

Formula	C₂₄H₂₃N₅O
Molecular Weight	397.47	CAS No.	811803-05-1
Solubility (25°C)*	In vitro	DMSO	79 mg/mL (198.75 mM)
		Ethanol	9 mg/mL (22.64 mM)
		Water	Insoluble
* <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.)

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Biological Activity

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.

Targets

VEGFR2 ^[1] (Cell-free assay)	RET ^[1] (Cell-free assay)
1 nM	13 nM

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].　

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HUVEC Concentrations 0.1 and 1 μM Incubation Time 72 h Method 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 37℃ and then washed with 1% acetic acid. Tris was added to dissolve the complex, and the optical density was measured at 520 nm.
Animal Study:^{^[1]}	Animal Models tumor xenograft model (NCI-H460 human lung tumors, HCT 116 human colon tumors, or SGC-7901 human gastric tumors; BALB⁄cA nude mice) Dosages 50, 100 and 200 mg/kg Administration by oral gavage

Cell Assay:^{^[1]}

Cell lines
HUVEC
Concentrations
0.1 and 1 μM
Incubation Time
72 h
Method
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 37℃ and then washed with 1% acetic acid. Tris was added to dissolve the complex, and the optical density was measured at 520 nm.

Animal Study:^{^[1]}

Animal Models
tumor xenograft model (NCI-H460 human lung tumors, HCT 116 human colon tumors, or SGC-7901 human gastric tumors; BALB⁄cA nude mice)
Dosages
50, 100 and 200 mg/kg
Administration
by oral gavage

References

[1] Tian S, et al. Cancer Sci. 2011, 102(7):1374-80.

Selleck's Apatinib has been cited by 28 publications

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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