SU015  (Synonyms: DOTA-RGDfK dimer)

SU015 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) 可抑制 HUVEC 细胞通过 αvβ3 介导的与纤维蛋白原的黏附作用，其 IC₅₀ 为 0.21 μM^[1]。
SU015 (0.1-100 μM; 15 min) 可抑制转染 293/β3 的 CHO 细胞通过 αvβ3 介导的与纤维蛋白原的黏附作用，其 IC₅₀ 为 0.32 μM^[1]。
SU015 (0.1-100 μM; 15 min) 可抑制活化血小板通过 αvβ3 介导的与骨桥蛋白的黏附作用，其 IC₅₀ 为 0.63 μM^[1]。
SU015 (0.1-100 μM; 15 min) 以 0.50 μM 的 IC₅₀ 抑制 SK-BR-3 细胞通过 αvβ5 介导的与玻连蛋白的黏附^[1]。

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

SU015 (3.75-7.5 μg；局部) 可强效抑制成纤维细胞生长因子 2 诱导的鸡胚尿囊膜模型血管生成^[1]。

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)

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.  [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]