Name: Cyclo(RGDyK)
Price: 286.00 USD

- Overview
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    Background
    
    Target: αVβ3 integrin
    IC50: 20 nM
    Cyclo(RGDyK) is a selective and potent αVβ3 integrin inhibitor with IC50 value of 20 nM [1]. The αVβ3 integrin, expressed on various malignant human tumors and on endothelial cells, plays an important role in tumor-induced angiogenesis and tumor metastasis. Therefore, αVβ3 integrin is a potential therapeutic target for tumor disease. Inhibition of αVβ3 integrin by αVβ3 antagonists not only blocked blood vessel formation but further led to tumor regression [1].
    In vitro: Cyclo(RGDyK) conjugation facilitated intracellular drug delivery of polymeric micelles to neovasculature (HUVECs) and tumor cells in which integrin is overexpressed [2]. In addition, Cyclo(RGDyK) showed high affinity and selectivity for αVβ3 integrin over αVβ5 and αIIbβ3 [1].
    In vivo: Cyclo(RGDyK) (1 nM, i.v. injection) blocked the increase of αVβ3 integrin expression in the intima of the left stenotic carotid artery of apoE-/- mice [2].
    
    1. Haubner R, Wester HJ, Burkhart F, Senekowitsch-Schmidtke R, Weber W, Goodman SL, et al. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J Nucl Med. 2001;42(2):326-36.
    2. Yin J, Li Z, Yang T, Wang J, Zhang X, Zhang Q. Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature. J Drug Target. 2011;19(1):25-36.
- Properties
  - Alternative Name
    
    2,2,2-trifluoroacetic acid compound with 2-((1Z,2S,3Z,5R,6Z,8S,9Z,11S,12Z)-8-(4-aminobutyl)-11-(3-guanidinopropyl)-3,6,9,12,15-pentahydroxy-5-(4-hydroxybenzyl)-1,4,7,10,13-pentaazacyclopentadeca-3,6,9,12,15-pentaen-2-yl)acetic acid (2:1)
    
    CAS Number
    
    250612-42-1
    
    Molecular Formula
    
    C31H43F6N9O12
    
    Molecular Weight
    
    847.72
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; ≥50.2 mg/mL in H2O with ultrasonic; ≥6.347 mg/mL in DMSO with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Cyclo(RGDyK)

Cyclo(RGDyK)

Background

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