A cyclic peptide ligand of αVβ3 integrin
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Cyclo(RGDyK) (trifluoroacetate salt)

Item No. 35173

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclo(L-arginylglycyl-L-α-aspartyl-D-tyrosyl-L-lysyl), trifluoroacetate salt
Synonyms
  • c(RGDyK)
  • cyclic-L-Arg-L-Gly-L-Asp-D-Tyr-L-Lys
Molecular Formula
C27H41N9O8 • XCF3COOH
Formula Weight
619.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Ethanol: solubleWater: soluble
λmax
225 nm
SMILES
O=C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N1)=O)CC(O)=O)=O)=O)CCCNC(N)=N)=O)CCCCN)[C@H]1CC2=CC=C(C=C2)O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C27H41N9O8.C2HF3O2/c28-10-2-1-4-18-24(42)34-17(5-3-11-31-27(29)30)23(41)32-14-21(38)33-20(13-22(39)40)26(44)36-19(25(43)35-18)12-15-6-8-16(37)9-7-15;3-2(4,5)1(6)7/h6-9,17-20,37H,1-5,10-14,28H2,(H,32,41)(H,33,38)(H,34,42)(H,35,43)(H,36,44)(H,39,40)(H4,29,30,31);(H,6,7)/t17-,18-,19+,20-;/m0./s1
InChi Key
KTQFOJMRRQLTAN-HXSCNMCGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    Cyclo(RGDyK) is a cyclic peptide ligand of αVβ3 integrin (IC50 = 37.5 nM) that contains the αVβ3 integrin-binding sequence arginine-glycine-aspartate (RGD).1 It has been conjugated to radiolabels or fluorescent probes for the visualization of αVβ3-mediated neoangiogenesis or optical imaging of αVβ3-expressing tumors in live mice.2,1 Cyclo(RGDyK) has also been conjugated to the DNA topoisomerase I inhibitor SN38 (Item No. 15632) and an SN38-releasing trigger moiety to form a prodrug that targets cells overexpressing αVβ3 integrin and induces cytotoxicity in KB human cervical carcinoma cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, X., Conti, P.S., and Moats, R.A. In vivo near-infrared fluorescence imaging of integrin αvβ3 in brain tumor xenografts. Cancer Res. 64(21), 8009-8014 (2004).

    2. van Hagen, P.M., Breeman, W.A., Bernard, H.F., et al. Evaluation of a radiolabelled cyclic DTPA-RGD analogue for tumour imaging and radionuclide therapy. Int. J. Cancer 90(4), 186-198 (2000).

    3. Huang, B., Desai, A., Tang, S., et al. The synthesis of a c(RGDyK) targeted SN38 prodrug with an indolequinone structure for bioreductive drug release. Org. Lett. 12(7), 1384-1387 (2010).