Apatinib

Catalog No.S2221 Synonyms: YN968D1

Apatinib 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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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.
Targets
VEGFR2 [1] RET [1] c-Kit [1] c-Src [1] PDGFRα [1]
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]

Protocol

Animal Research:[1]
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
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.

Chemical Information

Molecular Weight 493.58
Formula

C25H27N5O4S

CAS No. 811803-05-1
Storage powder
in solvent
Synonyms YN968D1

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03042611 Not yet recruiting Gastric Cancer|Gastric Adenocarcinoma LSK BioPartners Inc. February 7, 2017 Phase 3
NCT02980809 Not yet recruiting Small Cell Lung Cancer First Hospitals affiliated to the China PLA General Hospital March 2017 Phase 2
NCT03029013 Recruiting Cervical Cancer Third Military Medical University January 2017 --
NCT03020979 Not yet recruiting Malignant Ascites|Apatinib First Affiliated Hospital Bengbu Medical College January 2017 Phase 2
NCT03026881 Not yet recruiting Recurrent and Metastatic Gastric Cancer Jiangsu HengRui Medicine Co., Ltd.|Affiliated Hospital of Academy of Military Medical Sciences,China January 2017 Phase 1
NCT02995187 Not yet recruiting Small Cell Lung Cancer Chinese Academy of Medical Sciences December 2016 Phase 2

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID