Home Protein Tyrosine Kinase VEGFR inhibitor - c-RET inhibitor - c-Kit inhibitor - Src inhibitor - Autophagy activator - Apoptosis related activator Apatinib For research use only.

Apatinib

Synonyms: Rivoceranib, YN968D1

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.

Apatinib Chemical Structure

Apatinib Chemical Structure

CAS: 811803-05-1

Selleck's Apatinib has been cited by 22 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-VEGFR2 / VEGFR2 / p-ERK / ERK PI3K / p-PI3K / mTOR / p-mTOR / AKT / p-AKT Beclin 1 / Atg7 / p62 / LC3-I / LC3-II 29490645
Growth inhibition assay Cell viability 29490645
In Vivo
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].　
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05839197 Recruiting Macrotrabecular Massive Hepatocellular Carcinoma Wan-Guang Zhang|Tongji Hospital May 5 2023 Phase 2
NCT05742750 Not yet recruiting Locally Advanced Biliary Tract Cancer|Metastatic Biliary Tract Cancer Sun Yat-sen University|Jiangsu Hengrui Pharmaceutical Co. Ltd. March 1 2023 Phase 1|Phase 2
NCT05287360 Completed Healthy Elevar Therapeutics December 30 2021 Phase 1
NCT03743428 Suspended Colorectal Neoplasms Shenzhen People''s Hospital October 22 2020 Not Applicable
NCT04517357 Unknown status Relapsed Ovarian Cancer Jiangsu HengRui Medicine Co. Ltd. October 16 2020 Phase 2

Chemical lnformation & Solubility

Molecular Weight 397.47 Formula

C24H23N5O
CAS No. 811803-05-1 SDF --
Smiles O=C(NC1=CC=C(C=C1)C2(CCCC2)C#N)C3=C(NCC4=CC=NC=C4)N=CC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 79 mg/mL ( (198.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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