Apatinib (YN968D1) mesylate
For research use only.
Catalog No.S2221 Synonyms: Rivoceranib mesylate
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
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|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.|
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.  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. 
|In vivo||Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner.  Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model.  Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. |
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.
|In vitro||DMSO||22 mg/mL (44.57 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* 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.
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|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
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)
*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).
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 )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
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Frequently Asked Questions
How to reconstitute the compound S2221 for in vivo studies?
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.