[CAS NO. 262438-43-7] ATN-161 (Ac-PHSCN-NH2)
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PRODUCTS SPECIFICATIONS [262438-43-7]
Store
Catalog
SLK-S8454
Brand
Selleck
CAS
262438-43-7
DESCRIPTION [262438-43-7]
Overview
| MDL | MFCD30478885 |
|---|---|
| Molecular Weight | 597.64 |
| Molecular Formula | C23H35N9O8S |
| 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 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
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 |
| 50 mM | - | - | - |
Description
ATN-161 (Ac-PHSCN-NH2) is a novel small peptide antagonist of . It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
In vitro
ATN-161 interacts with the N-terminus of the β1-domain of integrin α5β1, which may lock this integrin in an inactive conformation. ATN-161 treatment up to 100 μmol/L shows no significant effect on tumor cell proliferation compared with the vehicle-treated control group of cells. However, ATN-161 significantly inhibits MAPK phosphorylation with maximal effects observed at 20 μmol/L of ATN-161 after 30 minutes of treatment.
In vivo
ATN-161 (Ac-PHSCN-NH2), a 5-mer capped peptide derived from the synergy region of fibronectin that binds to α5β1 and αvβ3 in vitro, blocks breast cancer growth and metastasis. Treatment with ATN-161 causes a significant dose-dependent decrease in tumor volume and either completely blocked or caused a marked decrease in the incidence and number of skeletal as well as soft tissue metastases. Treatment with ATN-161 results in a significant decrease in the expression of phosphorylated mitogen-activated protein kinase, microvessel density, and cell proliferation in tumors grown in vivo. ATN-161 is a peptide with a fairly short plasma half-life. compared with the plasma pharmacokinetics of ATN-161, It is cleared from the tumor with much slower kinetics supporting the hypothesis that this peptide exerts its effects through a durable interaction with its target(s)in the tumor.
References
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