Apatinib mesylate

Catalog No.S2221 Synonyms: YN968D1

Apatinib mesylate Chemical Structure

Molecular Weight(MW): 493.58

Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 320 In stock
USD 970 In stock
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Purity & Quality Control

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Biological Activity

Description Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
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]

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
  • Formulation: 0.5% (w/v) carboxymethyl cellulose
  • 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 YN968D1

Bio Calculators

Molarity Calculator

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Dilution Calculator

Dilution Calculator

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

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The Serial Dilution Calculator Equation

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03075462 Recruiting Ovarian Cancer|Triple Negative Breast Cancer Jiangsu HengRui Medicine Co. Ltd.|Beijing Cancer Hospital March 9 2017 Phase 1
NCT03651219 Not yet recruiting Small Cell Lung Cancer Beijing Chest Hospital|Jiangsu HengRui Medicine Co. Ltd. September 8 2018 Phase 3
NCT03422445 Recruiting Advanced Melanoma Beijing Cancer Hospital January 8 2018 Phase 2
NCT03243643 Recruiting Advanced Cancer Jiangsu Hansoh Pharmaceutical Co. Ltd. August 8 2017 Phase 1
NCT03251443 Recruiting Intrahepatic Cholangiocarcinoma|Second-line Treatment Peking Union Medical College Hospital|Jiangsu HengRui Medicine Co. Ltd. August 8 2017 Phase 3
NCT03521219 Recruiting Intrahepatic Cholangiocarcinoma The First Affiliated Hospital of Zhengzhou University|Jiangsu HengRui Medicine Co. Ltd. February 7 2018 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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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.

VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID