Chemical Property of N-(4-(1-Cyanocyclopentyl)phenyl)-2-((pyridin-4-ylmethyl)amino)nicotinamide
Chemical Property:
- Boiling Point:578.2±50.0 °C(Predicted)
- PKA:11.93±0.70(Predicted)
- PSA：90.70000
- Density:1.27
- LogP:4.82238
- XLogP3:4.1
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:6
- Exact Mass:397.19026037
- Heavy Atom Count:30
- Complexity:608
- Purity/Quality:
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99% *data from raw suppliers
Apatinib *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4
- Recent ClinicalTrials:Efficacy and Safety of Maintenance Apatinib Combined With Pemetrexed in Advanced Non-squamous Non-small Cell Lung Cancer Patients
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Description
Apatinib mesylate, discovered by Advenchen Laboratories (United
States of America, USA) and co-developed by Jiangsu Hengrui
Medicine Co. Ltd (China), was approved by the Chinese Food and
Drug Administration (CFDA) in October 2014 for the treatment of
metastatic gastric carcinoma. Apatinib mesylate is an oral tyrosine
kinase inhibitor that selectively inhibits the vascular
endothelial growth factor receptor 2 (VEGFR2), which prevents new blood vessel formation selectively in tumor tissue. Apatinib
has shown inhibition of the VEGF signaling pathway with an IC50
value of 1 nM for VEGFR-2 in in vitro enzyme experiments. A
multicenter phase II study of apatinib is underway with patients
in non-triple-negative metastatic breast cancer trials. Non-clinical
studies concluded that apatinib may reverse the ATP-binding
cassette subfamily B member 1 and subfamily G member 2
(ABCB1- and ABCG2, respectively)-mediated multidrug resistance
which allows cancer cells to circumvent certain conventional antineoplastic
drugs, suggesting that apatinib could be effective as a
combination therapy. Apatinib is a tyrosine kinase inhibitor that potently suppresses the kinase activity of vascular endothelial growth factor 2 (VEGFR2; IC50 = 1 nM). It is less effective against c-kit (IC50 = 429 nM), Ret (IC50 = 13 nM), and c-src (IC50 = 53 nM) and does not inhibit EGFR, Her-2, or FGFR1 (IC50s = >10 μM). Apatinib has been shown to inhibit the proliferation, migration, and tube formation of human umbilical vein endothelial cells stimulated by fetal bovine serum and, either alone, or in combination with chemotherapeutic agents, prevented the growth of several established human tumor xenograft models.
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Uses
Apatinib (YN968D1) is a small-molecule selective multitargeted tyrosine kinase inhibitor with an IC50 of 2.43 nM for the inhibition of VEGFR2.
