Apatinib

Catalog No.S5248 Synonyms: YN968D1

Apatinib Chemical Structure

Molecular Weight(MW): 397.47

Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.

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Biological Activity

Description Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.
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

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • 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)
  • Formulation: 0.5% (w⁄v) carboxymethyl cellulose and 5%(w⁄v) glucose solution
  • Dosages: 50, 100 and 200 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (198.75 mM)
Ethanol 10 mg/mL (25.15 mM)
Water 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.

Chemical Information

Molecular Weight 397.47
Formula

C24H23N5O

CAS No. 811803-05-1
Storage powder
in solvent
Synonyms YN968D1

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03193814 Not yet recruiting Colorectal Cancer|Chemotherapy|Angiogenesis Wuhan Union Hospital China December 1 2019 Phase 2
NCT03193814 Not yet recruiting Colorectal Cancer|Chemotherapy|Angiogenesis Wuhan Union Hospital China December 1 2019 Phase 2
NCT03878472 Not yet recruiting Gastric Cancer Qilu Hospital of Shandong University April 1 2019 Phase 2
NCT03878472 Not yet recruiting Gastric Cancer Qilu Hospital of Shandong University April 1 2019 Phase 2
NCT03801200 Not yet recruiting NSCLC Hubei Cancer Hospital April 2019 Phase 2
NCT03801200 Not yet recruiting NSCLC Hubei Cancer Hospital April 2019 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID