Tyr3-Octreotate 

Tyr3-Octreotate is a ligand for somatostatin receptor subtype 2 (sst2), with an IC₅₀ value of 1.3 nM against sst2 when labeled with [¹¹¹In-DTPA], and an IC₅₀ value of 1.6 nM against sst2 when labeled with [⁹⁰Y-DOTA]. Radiolabeled Tyr3-Octreotate generates cell-associated radioactivity, and acts as both a tumor growth inhibitor and a tumor cytotoxic agent. When radiolabeled with ¹⁷⁷Lu or ⁹⁰Y, Tyr3-Octreotate serves as a peptide receptor radionuclide therapy (PRRT) analog. Tyr3-Octreotate can be used in studies related to pancreatic tumors^[1].

Unlabeled Tyr³-octreotate (3×10^-8-3×10^-7 M; 1 hour) minimally reduces colony formation in CA20948 rat pancreatic tumor cells, with only a 5-10% reduction in cell survival^[1].

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

¹⁷⁷Lu-labeled Tyr3-Octreotate (277.5-555 MBq; single administration, two dose levels) cures rats bearing small CA20948 tumors, and achieves a maximum cure rate of 50% in rats bearing larger tumors^[1].

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

1049.22

C₄₉H₆₄N₁₀O₁₂S₂

302794-43-0

Solid

White to off-white

{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Thr-Cys-Thr (Disulfide bridge: Cys2-Cys7)

{d-Phe}-CY-{d-Trp}-KTCT (Disulfide bridge: Cys2-Cys7)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Capello A, et al. Tyr3-octreotide and Tyr3-octreotate radiolabeled with 177Lu or 90Y: peptide receptor radionuclide therapy results in vitro. Cancer Biother Radiopharm. 2003 Oct;18(5):761-8.  [Content Brief]