250612-06-7
Chemical Structure
SU015
Synonym(s): DOTA-RGDfK dimer
- CAS No.: 250612-06-7
- Formula:C75H113N23O23
- Molecular Weight:1704.84
IUPAC Name: 2,2',2''-(10-(2-(((S)-1,5-bis((4-((2S,5S,11S,14R)-14-benzyl-11-(carboxymethyl)-5-(3-guanidinopropyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)butyl)amino)-1,5-dioxopentan-2-yl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
InChIKey: PBVFRFXAHGNWCI-TYIUZRSTSA-N
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)CCCCNC([C@H](CCC(NCCCC[C@@H]2NC([C@H](NC([C@@H](NC(CNC([C@@H](NC2=O)CCCNC(N)=N)=O)=O)CC(O)=O)=O)CC3=CC=CC=C3)=O)=O)NC(CN4CCN(CCN(CCN(CC4)CC(O)=O)CC(O)=O)CC(O)=O)=O)=O)[C@H]1CC5=CC=CC=C5
Biological Activity: SU015 (DOTA-RGDfK dimer) is a Integrin αvβ5 and αvβ3 antagonist. SU015 exhibits comparable affinity for αvβ5 and αvβ3, with relatively higher potency and specificity compared to other integrins. SU015 inhibits αvβ3-mediated cell adhesion to fibrinogen, αvβ3-mediated adhesion of activated platelets to osteopontin, and αvβ5-mediated cell adhesion to vitronectin. SU015 shows potent inhibitory effects on FGF2-induced angiogenesis in the CAM model. SU015 carries a linker arm available for radioisotope conjugation, and acts as a target-specific radioreagent when labeled with 90Y (i.e., RP697) or 177Lu (i.e., RP688). SU015 can be used in studies related to tumor metastasis and tumors[1][2].
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SU015 | SU015 (DOTA-RGDfK dimer) is a Integrin αvβ5 and αvβ3 antagonist. SU015 exhibits comparable affinity for αvβ5 and αvβ3, with relatively higher potency and specificity compared to other integrins. SU015 inhibits αvβ3-mediated cell adhesion to fibrinogen, αvβ3-mediated adhesion of activated platelets to osteopontin, and αvβ5-mediated cell adhesion to vitronectin. SU015 shows potent inhibitory effects on FGF2-induced angiogenesis in the CAM model. SU015 carries a linker arm available for radioisotope conjugation, and acts as a target-specific radioreagent when labeled with 90Y (i.e., RP697) or 177Lu (i.e., RP688). SU015 can be used in studies related to tumor metastasis and tumors. | |||||||||||||||||||||
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References
- [1]. Wright T. αv Integrin Affinity/Specificity and Antiangiogenesis Effect of a Novel Tetraaza Cyclic Peptide Derivative, SU015, in Various Species: Retraction. J Cardiovasc Pharmacol. 2023 Aug 23. [Content Brief]
- [2]. Liu S, et al. (90)Y and (177)Lu labeling of a DOTA-conjugated vitronectin receptor antagonist useful for tumor therapy. Bioconjug Chem. 2001;12(4):559-568. [Content Brief]
