Apatinib - CAS 1218779-75-9
Catalog number: 1218779-75-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H27N5O4S
Molecular Weight:
493.58
COA:
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Targets:
VEGFR
Description:
Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.
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Purity:
>98%
Synonyms:
YN968D1
MSDS:
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1.Apatinib: A novel receptor tyrosine kinase inhibitor for the treatment of gastric cancer.
Roviello G1, Ravelli A2, Polom K3, Petrioli R4, Marano L5, Marrelli D6, Roviello F3, Generali D7. Cancer Lett. 2016 Mar 28;372(2):187-91. doi: 10.1016/j.canlet.2016.01.014. Epub 2016 Jan 18.
Metastatic gastric cancer is a lethal disease characterized by a very short overall survival, underlining a critical need of new therapeutic options. Unfortunately, although several molecular targets have been investigated, only very few recently approved agents, such as trastuzumab in the HER2-positive setting and ramucirumab, led to a clinical improvement in the outcome of metastatic gastric cancer patients. VEGF (vascular endothelial growth factor) is one of the most potent angiogenic factors and is a signalling molecule secreted by many solid tumours. Since high VEGF expression is one of the characteristic features of gastric carcinomas, targeting VEGF is therefore considered as a promising therapeutic strategy for gastric cancer. In the scenario of possible new target therapies with particular regard to angiogenesis, apatinib is a novel receptor tyrosine kinase inhibitor selectively targeting VEGFR-2. It is an orally-bioavailable agent currently being studied in several solid tumour types showing a promising activity in gastric cancer.
2.Randomized, Double-Blind, Placebo-Controlled Phase III Trial of Apatinib in Patients With Chemotherapy-Refractory Advanced or Metastatic Adenocarcinoma of the Stomach or Gastroesophageal Junction.
Li J1, Qin S1, Xu J1, Xiong J1, Wu C1, Bai Y1, Liu W1, Tong J1, Liu Y1, Xu R1, Wang Z1, Wang Q1, Ouyang X1, Yang Y1, Ba Y1, Liang J1, Lin X1, Luo D1, Zheng R1, Wang X1, Sun G1, Wang L1, Zheng L1, Guo H1, Wu J1, Xu N1, Yang J1, Zhang H1, Cheng Y1, Wang N1, J Clin Oncol. 2016 May 1;34(13):1448-54. doi: 10.1200/JCO.2015.63.5995. Epub 2016 Feb 16.
PURPOSE: There is currently no standard treatment strategy for patients with advanced metastatic gastric cancer experiencing progression after two or more lines of chemotherapy. We assessed the efficacy and safety of apatinib, a novel vascular endothelial growth factor receptor 2 tyrosine kinase inhibitor, in patients with advanced gastric or gastroesophageal junction adenocarcinoma for whom at least two lines of prior chemotherapy had failed.
3.Apatinib inhibits VEGF signaling and promotes apoptosis in intrahepatic cholangiocarcinoma.
Peng H1, Zhang Q2, Li J1, Zhang N3, Hua Y1, Xu L3, Deng Y4, Lai J5, Peng Z6, Peng B1, Chen M3, Peng S3, Kuang M1,7. Oncotarget. 2016 Mar 7. doi: 10.18632/oncotarget.7948. [Epub ahead of print]
Tumor cells co-express vascular endothelial growth factor (VEGF) and VEGF receptors (VEGFRs) that interact each other to support a self-sustainable cell growth. So far, this autocrine VEGF loop is not reported in human intrahepatic cholangiocarcinoma (ICC). Apatinib is a highly selective VEGFR2 inhibitor, but its effects on ICC have not been investigated. In this study, we reported that VEGF and phosphorylated VEGFR2 were expressed at a significantly high level in ICC patient tissues (P<0.05). In vitro, treating ICC cell lines RBE and SSP25 with recombinant human VEGF (rhVEGF) induced phosphorylation of VEGFR1 (pVEGFR1) and VEGFR2 (pVEGFR2); however, only the VEGFR2 played a role in the anti-apoptotic cell growth through activating a PI3K-AKT-mTOR anti-apoptotic signaling pathway which generated more VEGF to enter this autocrine loop. Apatinib inhibited the anti-apoptosis induced by VEGF signaling, and promoted cell death in vitro. In addition, Apatinib treatment delayed xenograft tumor growth in vivo.
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CAS 1218779-75-9 Apatinib

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