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ATN-161 TFA, the trifluoroacetic acid salt of ATN161, is a novel and potent small peptide inhibitor of the integrin α5β1 with potential anticancer activity. It inhibits the angiogenesis and growth of liver metastases in a murine model. ATN-161 acts by interacting with the N-terminus of the β1-domain of integrin α5β1, which may lock this integrin in an inactive conformation. Integrin α5β1 is expressed on activated endothelial cells and plays a critical role in tumor angiogenesis. Therefore, ATN-161 has potential anticancer activities.The combination of ATN-161 with 5-fluorouracil (5-FU) chemotherapy has shown enhanced antineoplastic effect.
| ln Vitro |
The combination of ATN-161 trifluoroacetate salt and 5-FU significantly reduced tumor cell proliferation compared to control and single-drug treatments (p<0.01). Furthermore, combination treatment resulted in a substantial increase in apoptotic (TUNEL-positive) tumor cells (p<0.03), whereas single-agent treatment did not raise TUNEL-positive tumor cells. Treatment with ATN-161 trifluoroacetate salt resulted in a significant reduction (21% reduction) in EC numbers after 48 hours of incubation compared to the control (p<0.03)[1]. ATN-161 trifluoroacetate salt inhibits VEGF-induced hCEC migration and capillary tube formation, but not proliferation. Starting from 100 nM, ATN-161 trifluoroacetate salt reduced the number of cell migration in response to VEGF in a dose-dependent manner (P<0.001 compared with the VEGF group) [2].
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| ln Vivo |
Treatment with ATN-161 trifluoroacetate salt significantly reduced tumor weight and vessel density in HT29 α5β1-negative human colon cancer xenografts, according to preliminary experiments [1]. The degree of inhibition of choroidal neovascularization (CNV) leakage and neovascularization that can be achieved by injecting ATN-161 trifluoroacetate salt following laser photocoagulation is comparable to that of AF564 [2].
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| References |
[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 |
| Molecular Formula |
C25H36F3N9O10S
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| Molecular Weight |
711.67
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| CAS # |
904763-27-5
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| Related CAS # |
ATN-161;262438-43-7
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| SMILES |
O=C(N)[C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([ C@H]1N(C(C)=O)CCC1)=O)CC2=CN= CN2)=O)CO)=O)CS)=O)CC(N)=O.O=C(O)C(F)(F)F
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| Chemical Name |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (14.05 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4051 mL | 7.0257 mL | 14.0515 mL | |
| 5 mM | 0.2810 mL | 1.4051 mL | 2.8103 mL | |
| 10 mM | 0.1405 mL | 0.7026 mL | 1.4051 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 ATN-453 binding to HUVECs can be competed by ATN-161.Clin Cancer Res.2008 Apr 1;14(7):2137-44. |
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ATN-161 inhibits angiogenesis in a Matrigel plug model.Clin Cancer Res.2008 Apr 1;14(7):2137-44. |
ATN-453 localizes to neovessels in 3LL tumors grown in Matrigelin vivo.Clin Cancer Res.2008 Apr 1;14(7):2137-44. |
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 Effect of ATN-161 on MDA-MB 231-GFP breast cancer micrometastases.Mol Cancer Ther.2006 Sep;5(9):2271-80 |
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