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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
ATN-161 is a novel and potent small peptide inhibitor of the integrin α5β1, it inhibits the angiogenesis and growth of liver metastases in a murine model. ATN-161 interacts 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 |
When compared to control and single-agent therapy, the combination of ATN-161 plus 5-FU significantly reduces tumor cell proliferation (p<0.01). Furthermore, apoptotic (TUNEL-positive) tumor cells are significantly increased by combination therapy (p <0.03), while no increase in TUNEL-positive tumor cells is observed with single-agent therapy. After 48 hours of incubation, ATN-161 treatment significantly lowers the EC number (21% decrease) in comparison to the control group (p<0.03) [1]. ATN-161 did not stop proliferation in hCECs, but it did prevent VEGF-induced migration and capillary tube formation. Starting at 100 nM (P <0.001 vs. VEGF group), ATN-161 reduces the number of cells migrating in response to VEGF in a dose-dependent manner[2].
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ln Vivo |
Preliminary studies using human colon cancer xenografts (HT29) lacking α5β1 demonstrate that ATN-161 treatment dramatically lowers tumor weight and vessel density[1]. Following laser photocoagulation, injection of ATN-161 inhibits choroidal neovascularization (CNV) leakage and neovascularization to a degree comparable to that of AF564[2].
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Animal Protocol |
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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 |
C23H35N9O8S
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Molecular Weight |
597.64
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CAS # |
262438-43-7
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Related CAS # |
ATN-161 trifluoroacetate salt;904763-27-5
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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
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Chemical Name |
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Synonyms |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6732 mL | 8.3662 mL | 16.7325 mL | |
5 mM | 0.3346 mL | 1.6732 mL | 3.3465 mL | |
10 mM | 0.1673 mL | 0.8366 mL | 1.6732 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. th> |
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ATN-161 inhibits angiogenesis in a Matrigel plug model.Clin Cancer Res.2008 Apr 1;14(7):2137-44. td> |
ATN-453 localizes to neovessels in 3LL tumors grown in Matrigelin vivo.Clin Cancer Res.2008 Apr 1;14(7):2137-44. td> |
Effect of ATN-161 on MDA-MB 231-GFP breast cancer micrometastases.Mol Cancer Ther.2006 Sep;5(9):2271-80. td> |