SU015  (Synonyms: DOTA-RGDfK dimer)

SU015 (DOTA-RGDfK dimer) is a Integrin α_vβ₅ and α_vβ₃ antagonist. SU015 exhibits comparable affinity for α_vβ₅ and α_vβ₃, with relatively higher potency and specificity compared to other integrins. SU015 inhibits α_vβ₃-mediated cell adhesion to fibrinogen, α_vβ₃-mediated adhesion of activated platelets to osteopontin, and α_vβ₅-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].

SU015 (0.1-100 μM; 15 min) inhibits αvβ3-mediated adhesion of HUVEC cells to fibrinogen, with an IC₅₀ of 0.21 μM^[1].
SU015 (0.1-100 μM; 15 min) inhibits αvβ3-mediated adhesion of 293/β3-transfected CHO cells to fibrinogen, with an IC₅₀ of 0.32 μM^[1].
SU015 (0.1-100 μM; 15 min) inhibits the αvβ3-mediated adhesion of activated human platelets to osteopontin, with an IC₅₀ of 0.63 μM^[1].
SU015 (0.1-100 μM; 15 min) inhibits αvβ5-mediated adhesion of SK-BR-3 cells to vitronectin with an IC₅₀ of 0.50 μM^[1].

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

SU015 (3.75-7.5 μg; local administration) potently inhibits fibroblast growth factor 2-induced angiogenesis in the chick chorioallantoic membrane model^[1].

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

1704.84

C₇₅H₁₁₃N₂₃O₂₃

250612-06-7

DOTA-di(Arg-Gly-Asp-{D-Phe}-Lys)

DOTA-di(RGD-{D-Phe}-K)

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.

  [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.