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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.
| Targets |
α5β1 Integrin
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| 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].
Inhibits the adhesion of human umbilical vein endothelial cells (HUVECs) to fibronectin. The mechanism is that ATN - 161 can block the binding of integrin α5β1 to fibronectin, thereby inhibiting cell adhesion, which is detected by a cell adhesion assay [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].
- When combined with 5 - FU, it can reduce colorectal liver metastases and improve the survival rate of mice. In a mouse model of colon cancer, ATN - 161 is administered subcutaneously at a dose of 100 μg per mouse per day, and 5 - FU is continuously infused intravenously. As a result, the number of liver metastases is significantly reduced, and the survival time of mice is prolonged [1] - Inhibits angiogenesis in vivo. In a mouse model, after subcutaneous injection of ATN - 161, it can reduce the formation of new blood vessels in the tumor, which is evaluated by measuring the micro - vessel density of the tumor tissue [2] |
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| Cell Assay |
- When combined with 5 - FU, it can reduce colorectal liver metastases and improve the survival rate of mice. In a mouse model of colon cancer, ATN - 161 is administered subcutaneously at a dose of 100 μg per mouse per day, and 5 - FU is continuously infused intravenously. As a result, the number of liver metastases is significantly reduced, and the survival time of mice is prolonged [1]
- Inhibits angiogenesis in vivo. In a mouse model, after subcutaneous injection of ATN - 161, it can reduce the formation of new blood vessels in the tumor, which is evaluated by measuring the micro - vessel density of the tumor tissue [2] |
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| Additional Infomation |
ATN - 161 is a pentapeptide derived from the synergistic region of fibronectin. It exerts anti - tumor and anti - angiogenesis effects by blocking the integrin - mediated signaling pathway, mainly targeting integrin α5β1. It can block the binding of integrin α5β1 to fibronectin, inhibit cell adhesion, and then inhibit tumor angiogenesis and the metastasis of cancer cells
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| Molecular Formula |
C25H36F3N9O10S
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| Molecular Weight |
711.67
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| Exact Mass |
711.225
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| Elemental Analysis |
C, 42.19; H, 5.10; F, 8.01; N, 17.71; O, 22.48; S, 4.50
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| CAS # |
904763-27-5
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| Related CAS # |
ATN-161;262438-43-7; ATN-161 trifluoroacetate salt;904763-27-5; 904763-50-4 (mesylate); 904763-42-4 (HCl); 904763-58-2 (acetate); 904763-74-2 (sulfate)
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| PubChem CID |
92044380
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| Sequence |
Ac-Pro-His-Ser-Cys-Asn-NH2 TFA;
N-acetyl-L-prolyl-L-histidyl-L-seryl-L-cysteinyl-L-asparaginamide trifluoroacetic acid
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| SequenceShortening |
PHSCN
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
48
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| Complexity |
1100
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CN=CN2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(=O)N)C(=O)N.C(=O)(C(F)(F)F)O
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| InChi Key |
MCVJOWHOEOLJGI-LQCLSJOXSA-N
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| InChi Code |
InChI=1S/C23H35N9O8S.C2HF3O2/c1-11(34)32-4-2-3-17(32)23(40)29-14(5-12-7-26-10-27-12)20(37)30-15(8-33)21(38)31-16(9-41)22(39)28-13(19(25)36)6-18(24)35;3-2(4,5)1(6)7/h7,10,13-17,33,41H,2-6,8-9H2,1H3,(H2,24,35)(H2,25,36)(H,26,27)(H,28,39)(H,29,40)(H,30,37)(H,31,38);(H,6,7)/t13-,14-,15-,16-,17-;/m0./s1
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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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