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  4. ATN-161

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

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ATN-161 Chemical Structure

ATN-161 Chemical Structure

CAS No. : 262438-43-7

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Based on 8 publication(s) in Google Scholar

Other Forms of ATN-161:

ATN-161 Related Antibodies

Top Publications Citing Use of Products

View All Integrin Isoform Specific Products:

View All Isoforms
αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

Integrin α5β1[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ATN-161 Related Antibodies
In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

597.64

Formula

C23H35N9O8S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C[C@@H](C(N)=O)NC([C@H](CS)NC([C@H](CO)NC([C@H](CC1=CNC=N1)NC([C@H]2N(C(C)=O)CCC2)=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (41.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 10 mg/mL (16.73 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[1]

Ninety-six well microtiter plates are coated with fibronectin(20 μg/mL) overnight at 4°C. HUVECs are then trypsinized as described above and resuspended in 1% FBS-MEM for cell counting. Cell suspensions with 10,000 cells/mL are prepared in serum-reduced conditions by using 1% FBS-MEM, or 1% FBS-MEM containing either ATN-161 (1 μM) or ATN-163 (scrambled peptide as control; 1μM) to allow interference by the peptide during the ligand binding process (i.e., binding of α5β1 to fibronectin). Cells are thereafter plated into each well (2,000 cells/well in 200 μL) of the fibronectin-coated 96-well plates. Cells are incubated at 37°C for 48 hr under these serum-reduced conditions in order to evaluate effects of ATN-161 on EC survival and proliferation. Estimation of cell number is performed by adding 40 μL MTT to each well and incubating for 2 hr at 37°C. Media is then removed, cells are solubilized in 100 μL DMSO and optical density is measured at 560 nm. Experiments are performed in triplicate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Eight-week-old male BALB/c mice are acclimated for 1 week while caged in groups of 5. Mice are fed a diet of animal chow and water ad libitum throughout the experiment. CT-26 cells (10,000 cells in 50 μL HBSS) are injected into the spleens of 40 BALB/c mice to produce liver metastases. Mice are randomly assigned to 1 of 4 treatment groups (10 mice per group): (A) control (saline/saline), (B) 5-FU alone, (C) ATN-161 alone and (D) ATN-161 plus 5-FU. Body weight at randomization is similar among groups. Treatment with ATN-161 (100 mg/kg) or saline is started on day 4 after CT-26-cell injection and is administered every third day thereafter by intraperitoneal injection. In previous studies, administration of the peptide every third day has been shown to be adequate for sustained inhibition of integrin α5β1 activity. Mice are allowed to recover for 1 week from the surgical procedure and effects of anesthesia with pentobarbital (Nembutal, 50 mg/kg). On day 7, mice are anaesthetized again and osmotic pumps.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.6732 mL 8.3662 mL 16.7325 mL 41.8312 mL
5 mM 0.3346 mL 1.6732 mL 3.3465 mL 8.3662 mL
10 mM 0.1673 mL 0.8366 mL 1.6732 mL 4.1831 mL
15 mM 0.1115 mL 0.5577 mL 1.1155 mL 2.7887 mL
DMSO 20 mM 0.0837 mL 0.4183 mL 0.8366 mL 2.0916 mL
25 mM 0.0669 mL 0.3346 mL 0.6693 mL 1.6732 mL
30 mM 0.0558 mL 0.2789 mL 0.5577 mL 1.3944 mL
40 mM 0.0418 mL 0.2092 mL 0.4183 mL 1.0458 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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ATN-161 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ATN-161262438-43-7ATN161ATN 161IntegrinInhibitorinhibitorinhibit

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