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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- CAS No.: 250612-06-7
- Formule: C75H113N23O23
- Masse moléculaire:1704.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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αvβ3 |
αvβ5 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:10-day-old embryos[1]
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Dosage:3.75 μg; 7.5 μg
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Administration:topical application
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Result:Inhibited fibroblast growth factor-2-induced angiogenesis by 55% at 3.75 μg.
Inhibited fibroblast growth factor-2-induced angiogenesis by 88% at 7.5 μg.
Chemical Information
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CAS No. 250612-06-7
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Masse moléculaire 1704.84
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Formule C75H113N23O23
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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
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Synonyms
DOTA-RGDfK dimer
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Sequence
DOTA-di(Arg-Gly-Asp-{D-Phe}-Lys)
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Sequence Shortening
DOTA-di(RGD-{D-Phe}-K)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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