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:
Inquire
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.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
YN968D1
MSDS:
Inquire
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related VEGFR Products


AG28262
(CAS: 638216-89-4)

AG28262 is a bio-active chemical compound. It is a VEFG-r2 inhibitor and could cause an increase in serum ALT, due in part to both gene up-regulation.

CAS 443913-73-3 Vandetanib

Vandetanib
(CAS: 443913-73-3)

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

BRN-103
(CAS: 1346265-80-2)

BRN-103 can suppress the phosphorylation of vascular endothelial growth factor (VEGF) receptor 2. It can also inhibit the activations of AKT and eNOS. These res...

Fruquintinib
(CAS: 1194506-26-7)

Fruquintinib, also known as HMPL-013, is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential ...

CAS 288383-20-0 Cediranib dihydrochloride

Cediranib dihydrochloride
(CAS: 288383-20-0)

Cediranib (AZD-2171; tentative trade name Recentin) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.The drug is bei...

CAS 212141-51-0 Vatalanib dihydrochloride

Vatalanib dihydrochloride
(CAS: 212141-51-0)

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4.

BAW2881
(CAS: 861875-60-7)

BAW 2881 is a VEGFR (vascular endothelial growth factor receptor) inhibitor (IC50 = 0.82, 0.037, and 0.42 µM for VEGFR1, 2, and 3, respectively).It can inhibit ...

CAS 1019206-88-2 Regorafenib monohydrate

Regorafenib monohydrate
(CAS: 1019206-88-2)

Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311...

CAS 882531-87-5 R1530

R1530
(CAS: 882531-87-5)

R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (...

CAS 1430089-64-7 2,4-Pyrimidinediamine with linker

2,4-Pyrimidinediamine with linker
(CAS: 1430089-64-7)

2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

CAS 193001-14-8 ZM323881

ZM323881
(CAS: 193001-14-8)

ZM323881 inhibits VEGF-A, EGF and bFEF induced HUVEC cell proliferation with IC50 of 8 nM, 1.9 μM and 1.6 μM, respectively. ZM323881 (10 nM) abolishes VEGF-A-me...

CAS 15966-93-5 SU5408

SU5408
(CAS: 15966-93-5)

A potent, selective and cell-permeable inhibitor of VEGFR2 kinase(IC50= 70 nM) with little or no effect against receptors for platelet-derived growth factor, ep...

CAS 475108-18-0 Tivozanib

Tivozanib
(CAS: 475108-18-0)

Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplast...

JNJ 17029259
(CAS: 314267-57-7)

JNJ 17029259 is an selective, nanomolar inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2), blocks VEGF-stimulated mitogen-activated prot...

CAS 10537-47-0 Tyrphostin 9

Tyrphostin 9
(CAS: 10537-47-0)

Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.

CAS 286370-15-8 KRN633

KRN633
(CAS: 286370-15-8)

KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial ce...

CAS 168835-82-3 SU1498

SU1498
(CAS: 168835-82-3)

SU1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), and inhibits Flk-1 with an IC50 of value of 7...

CAS 228559-41-9 Ki8751

Ki8751
(CAS: 228559-41-9)

Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFRα and FGFR-2 (IC50 val...

CAS 1218779-75-9 Apatinib

Apatinib
(CAS: 1218779-75-9)

Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apa...

CAS 1018069-81-2 TG 100801 Hydrochloride

TG 100801 Hydrochloride
(CAS: 1018069-81-2)

TG 100801 is the prodrug of TG 100572, which is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kin...

Chemical Structure

CAS 1218779-75-9 Apatinib

Quick Inquiry

Verification code

Featured Items