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].

Assay
Methods Test Index PMID
Western blot
Beclin 1 / Atg7 / p62 / LC3-I / LC3-II ; 

PubMed: 30301881     


C643 and KHM-5M cells were treated with a serious concentration of apatinib for 24 h. The Beclin 1, ATG7, P62, LC3-II, and GAPDH expressions were detected by western blot.

PI3K / p-PI3K / mTOR / p-mTOR / AKT / p-AKT ; 

PubMed: 30301881     


C643 and KHM-5M cells treated with or without apatinib (20 μM) for 24 h, the expressions of total PI3K, phosphorylated PI3K, total AKT, phosphorylated AKT total mTOR, phosphorylated AKT, and GAPDH detected by western blot. 

p-VEGFR2 / VEGFR2 / p-ERK / ERK ; 

PubMed: 29490645     


Apatinib down-regulates the phosphorylation of VEGFR2 and its downstream signaling pathway in ALL cells. Jurkat (a), Nalm6 (b) cells were treated with 0, 10, 20 and 40 μM Apatinib for 48 h, respectively. The protein level of VEGFR2, p-VEGFR2 and its downstream signaling pathways were examined by western blotting. β-actin and GAPDH was used as a loading control in this experiment.

30301881 29490645
Growth inhibition assay
Cell viability; 

PubMed: 29490645     


Apatinib exhibits a dose- and time-dependent inhibition of proliferation of B and T-lineage ALL cell lines. B-lineage (a, b) and T-lineage ALL cells (c, d) were exposed to indicated concentrations of Apatinib for 48 or 72 h, and cell viability was subsequently determined by a CCK-8 kit.

29490645
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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03743428 Recruiting Drug: Apatinib Mesylate Tablets|Drug: Bevacizumab Injection Colorectal Neoplasms Shenzhen People''s Hospital October 22 2019 Not Applicable
NCT03878472 Not yet recruiting Drug: SHR1210|Drug: apatinib|Drug: S1 Gastric Cancer Qilu Hospital of Shandong University April 1 2019 Phase 2
NCT03816553 Recruiting Drug: SHR-1210|Drug: Apatinib Recurrent Cervical Carcinoma|Metastatic Cervical Cancer Sun Yat-sen University January 19 2019 Phase 2
NCT03764293 Not yet recruiting Drug: SHR-1210|Drug: Apatinib|Drug: Sorafenib Locally Advanced or Metastatic and Unresectable HCC Jiangsu HengRui Medicine Co. Ltd. January 2019 Phase 3
NCT03407976 Recruiting Drug: Apatinib|Drug: Pembrolizumab Advanced Malignancies|Urothelial Carcinoma|MSI-H or dMMR Solid Tumors|Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma University of Utah|LSK BioPartners Inc. June 19 2018 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID