In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO
40%PEG300
5%Tween80
50%ddH2O
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
3.950mg/ml
(9.94mM)
Taking the 1 mL working solution as an example, add 50 μL of 79 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO
95% Corn oil
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
0.450mg/ml
(1.13mM)
Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <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.)
Preparing Stock Solutions
Biological Activity
Description
Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signalling 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 (Cell-free assay)
RET (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. This compound suppressed the activities of Ret, c-kit and c-src with an IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. It had no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM. This chemical effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring.
In Vivo
In vivo, Apatinib alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumour xenograft models with little toxicity.
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.
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
https://pubmed.ncbi.nlm.nih.gov/21443688/
Sellecks Apatinib (YN968D1) Has Been Cited by 28 Publications
The Anti-Angiogenic Effect of Microbotox on Rosacea Is Due to the Suppressed Secretion of VEGF by Mast Cells Resulting From Internalization of the MRGPRX2 Receptor
[ Ann Dermatol, 2025, 37(4):228-240]
Targeting the VEGFR2 signaling pathway for angiogenesis and fibrosis regulation in neovascular age-related macular degeneration
[ Sci Rep, 2024, 14(1):25682]
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]
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
