Apatinib (YN968D1) mesylate

For research use only.

Catalog No.S2221 Synonyms: Rivoceranib mesylate

17 publications

Apatinib (YN968D1) mesylate Chemical Structure

CAS No. 1218779-75-9

Apatinib mesylate (YN968D1, Rivoceranib) 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 mesylate induces both autophagy and apoptosis.

Selleck's Apatinib (YN968D1) mesylate has been cited by 17 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Apatinib mesylate (YN968D1, Rivoceranib) 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 mesylate induces both autophagy and apoptosis.
Features Good anti-tumor effects for gastric and colorectal cancer compared with sorafenib and sunitinib.
VEGFR2 [1]
(Cell-free assay)
RET [1]
(Cell-free assay)
1 nM 13 nM
In vitro

Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. Apatinib can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. [1] Apatinib reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatinib significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [125I]iodoarylazidoprazosin in a concentration-dependent manner. [2]

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.

In vivo Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner. [1] Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model. [2] Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. [3]


Kinase Assay:


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Enzyme-linked immunosorbent assay:

A poly(glu, ala, tyr) 6:3:1 random copolymer is used as a tyrosine containing substrate solution. The substrate is stored as a 1 mg/mL stock in PBS at −20 °C and diluted 1 in 500 with PBS in order to coat 96 well plates (100 μL/well). Plates are coated on the day prior to assay, sealed with adhesive seals, and stored overnight at 4 °C. On the day of the assay, the substrate solution is discarded and the assay plate wells are washed once with PBST (PBS containing 0.05% v/v Tween 20) and once with Hepes buffer (50 mM, pH 7.4).Test compounds are diluted with 10% dimethylsulfoxide (DMSO) de-ionized water and 25 μL volumes transferred to wells in the washed assay plates. Manganese chloride solution (40 mM) containing 8 μM ATP is then added (25 μL) to all test wells. Control and blank wells, containing compound diluent and manganese chloride solution with and without ATP, respectively, are also included to determine the dynamic range of the assay. Freshly diluted enzyme (50 μL) is added to each well, and the plates incubated at room temperature for 20 min. The liquid is then discarded and the wells are washed twice with PBST. Mouse IgG anti-phosphotyrosine antibody diluted 1:6000 with PBST containing 0.5% (w/v) bovine serum albumin (BSA) is added (100 μL/well), and the plates incubated for 1h at room temperature before discarding the liquid and washing the wells twice with PBST. Horseradish peroxidase (HRP)-linked sheep anti-mouse Ig antibody diluted 1:500 with PBST containing 0.5% (w/v) BSA, is then added (100 μL/well) and the plates incubated for a further 1 h at room temperature before discarding the liquid and washing the wells twice with PBST. A 1 mg/mL solution of 2,2‘-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid is freshly prepared in 50 mM phosphate-citrate buffer (pH5.0) containing 0.03% (w/v) sodium perborate, and 100 μL added to each well. Plates are then incubated for 20−60 min at room temperature until the optical density value of control wells measured at 405 nm is approximately 1.0. IC50 values for compound enzyme inhibition are interpolated using Microcal Origin following subtraction of blank values.
Cell Research:


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  • Cell lines: HUVEC
  • Concentrations: ~25 μM
  • Incubation Time: 72 h
  • Method:

    The HUVEC are seeded into 96-well plates. After 24 h of incubation, cells are 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 are stained with 0.4% sulforhodamine B for 30 min at 37 °C and then washed with 1% acetic acid. Tris is added to dissolve the complex, and the optical density is measured at 520 n

    (Only for Reference)
Animal Research:


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  • Animal Models: Ls174t, HCT 116, SGC-7901, HT-29, A549, NCI-H460 xenografted BALB/cA nude mice
  • Dosages: 50, 100, 200 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 22 mg/mL (44.57 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC
For best results, use promptly after mixing.
6 mg/mL

* 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 493.58


CAS No. 1218779-75-9
Storage powder
in solvent
Synonyms Rivoceranib mesylate
Smiles C[S](O)(=O)=O.O=C(NC1=CC=C(C=C1)C2(CCCC2)C#N)C3=CC=CN=C3NCC4=CC=NC=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04517357 Recruiting Drug: Fluzoparib+Apatinib|Drug: Fluzoparib Relapsed Ovarian Cancer Jiangsu HengRui Medicine Co. Ltd. October 16 2020 Phase 2
NCT04659785 Recruiting Drug: Fluzoparib|Drug: Apatinib Small Cell Lung Cancer Extensive Stage Tianjin Medical University Second Hospital July 1 2020 Phase 1|Phase 2
NCT04476459 Recruiting Drug: Camrelizumab|Drug: Apatinib Diffuse Large B Cell Lymphoma|High-grade B-cell Lymphoma|Follicular Lymphoma Grade IIIb|Transformed Lymphoma|EBV-Positive DLBCL Nos|ALK-Positive Anaplastic Large Cell Lymphoma Huiqiang Huang|Sun Yat-sen University July 23 2020 Phase 1|Phase 2
NCT04335006 Recruiting Drug: Carelizumab|Drug: Nab-paclitaxel|Drug: Apatinib Breast Cancer|Triple Negative Breast Cancer Jiangsu HengRui Medicine Co. Ltd. July 14 2020 Phase 3

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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Frequently Asked Questions

  • Question 1:

    How to reconstitute the compound S2221 for in vivo studies?

  • Answer:

    We suggest the vehicle 0.5% CMC. In vehicle 0.5% CMC, the compound is not fully dissolved. However, the mixture is a stable suspension and can be used for oral gavage feeding.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID