Apatinib Inhibitor CAS No. 811803-05-1

Cat. No.	Name	Size	Price
KI3645	Apatinib	10 mg	$512
	Apatinib	50 mg	$1552
	Apatinib	200 mg	$4000

Chemical Characteristic

Product Name	Apatinib
CAS No.	811803-05-1
Molecular Weight	493.58
Formula	C₂₅H₂₇N₅O₄S
Chemical Name	N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide
Smiles	c1(c(cccn1)C(=O)Nc1ccc(cc1)C1(CCCC1)C#N)NCc1ccncc1
Chemical Structure
Documents	LCMS NMR

Biological activities

Apatinib, also known as YN968D1, is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) with IC50 of 1nM ^[1]. It is an orally bioavailable, small molecule agent which is thought to inhibit angiogenesis in cancer cells; specifically apatinib inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. This agent also mildly inhibits c-Kit and c-SRC tyrosine kinases. In vitro, Apatinib significantly inhibits proliferation stimulated by 20 ng/mL ^[2] VEGF (IC50 = 0.17?M). In vivo, Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model. Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts ^[3].

References

[1] Lin Y, Wang K, Hu C, et al. Elemene injection induced autophagy protects human hepatoma cancer cells from starvation and undergoing apoptosis. Evid Based Complement Alternat Med. 2014;2014:637528. [2] Ding J, Chen X, Gao Z, et al. Metabolism and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor apatinib in humans. Drug Metab Dispos. 2013,41(6):1195-210. [3] Tian S, Quan H, Xie C, et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011,102(7):1374-1380.

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