Apatinib

Catalog No.S2221

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

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Apatinib Chemical Structure

Apatinib Chemical Structure
Molecular Weight: 493.58

Validation & Quality Control

Quality Control & MSDS

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Product Description

Biological Activity

Description Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
Targets VEGFR2 [1] RET [1] c-Kit [1] c-Src [1] PDGFRα [1]

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IC50 1 nM 13 nM 429 nM 530 nM >1 μM
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]
Features Good anti-tumor effects for gastric and colorectal cancer compared with sorafenib and sunitinib.

Protocol(Only for 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.

Animal Study: [1]

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.
Solubility 0.5% CMC, 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tian S, et al. Cancer Sci, 2011, 102(7), 1374-1380.

[2] Mi YJ, et al. Cancer Res, 2010, 70(20), 7981-7991.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01726101 Recruiting Cancer Patients With Solid Tumors Bukwang Pharmaceutical, Co., Ltd.|LSK BioPartners Inc. April 2012 Phase 1|Phase 2
NCT01497704 Recruiting Cancer Patients With Solid Tumors LSK BioPartners Inc.|Bukwang Pharmaceutical, Co., Ltd. April 2012 Phase 1|Phase 2
NCT01653561 Completed Breast Neoplasms Fudan University|Jiangsu HengRui Medicine Co., Ltd. November 2011 Phase 2
NCT01531777 Recruiting Colorectal Cancer Jiangsu HengRui Medicine Co., Ltd.|Fudan University July 2011 Phase 2
NCT01287962 Active, not recruiting Non-small Cell Lung Cancer Sun Yat-sen University April 2011 Phase 3

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Chemical Information

Download Apatinib SDF
Molecular Weight (MW) 493.58
Formula

C25H27N5O4S

CAS No. 811803-05-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms YN968D1
Solubility (25°C) * In vitro DMSO 22 mg/mL (44 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 0.5% CMC 6 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.

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Tech Support & FAQs

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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