Apatinib (YN968D1) mesylate

Catalog No.S2221 Synonyms: Rivoceranib mesylate

For research use only.

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.

Apatinib (YN968D1) mesylate Chemical Structure

CAS No. 1218779-75-9

Selleck's Apatinib (YN968D1) mesylate has been cited by 20 publications

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Other VEGFR Products

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.
Targets
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]

Assay
Methods Test Index PMID
Western blot Beclin 1 / Atg7 / p62 / LC3-I / LC3-II ; PI3K / p-PI3K / mTOR / p-mTOR / AKT / p-AKT ; p-VEGFR2 / VEGFR2 / p-ERK / ERK 30301881 29490645
Growth inhibition assay Cell viability 29490645
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]

Protocol (from reference)

Kinase Assay:

[1]

  • 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:

[1]

  • 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:

[1]

  • 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
Formula

C25H27N5O4S

CAS No. 1218779-75-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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 2020 Not Applicable
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy Apatinib (YN968D1) mesylate | Apatinib (YN968D1) mesylate supplier | purchase Apatinib (YN968D1) mesylate | Apatinib (YN968D1) mesylate cost | Apatinib (YN968D1) mesylate manufacturer | order Apatinib (YN968D1) mesylate | Apatinib (YN968D1) mesylate distributor