ATN-161(Ac-PHSCN-NH2)是一由纤连蛋白的协同区域衍生出的五氨基酸短肽；具有抗肿瘤活性的β整合素拮抗剂。
CAS：262438-43-7
分子式：C23H35N9O8S
分子量：597.64
纯度：98%
存储：Store at -20°C

Background:

ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.

The combination of ATN-161 plus 5-FU significantly reduces tumor cell proliferation compared to control and single-agent therapy (p<0.01). In addition, combination therapy leads to a significant increase of apoptotic (TUNEL-positive) tumor cells (p<0.03), whereas single-agent therapy does not increase in TUNEL-positive tumor cells. ATN-161 treatment leads to a significant reduction in EC number (21% decrease) after a 48 hr incubation time compared to control (p<0.03)[1]. ATN-161 inhibites VEGF-induced migration and capillary tube formation in hCECs, but did not inhibit proliferation. ATN-161 decreases the number of cells migrating in response to VEGF in a dose-dependent manner starting at 100 nM (P<0.001 vs. VEGF group)[2].

The preliminary experiments with α5β1-negative human colon cancer xenografts (HT29) show that treatment with ATN-161 significantly reduces tumor weight and vessel density[1]. Injection of ATN-161 after laser photocoagulation inhibits choroidal neovascularization (CNV) leakage and neovascularization to an extent similar to AF564[2].

[1]. Stoeltzing O, et al. Inhibition of integrin alpha5beta1 function with a small peptide (ATN-161) plus continuous 5-FU infusion reduces colorectal liver metastases and improves survival in mice. Int J Cancer. 2003 Apr 20;104(4):496-503. [2]. Wang W, et al. The antiangiogenic effects of integrin alpha5beta1 inhibitor (ATN-161) in vitro and in vivo. Invest Ophthalmol Vis Sci. 2011 Sep 14;52(10):7213-20.