DOTA-Pep-1L TFA 

DOTA-Pep-1L TFA is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L TFA specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L TFA yields the isotopically labeled product [²²⁵Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L TFA can be used for PET imaging, tumor targeting and glioma research^[1][2].

DOTA-Pep-1L labeled with [²²⁵Ac] (5 μCi (185 kBq); i.t.; single stereotaxic injection) TFA doubles the mean survival time of mice bearing orthotopic U251 gliomas^[1].
DOTA-Pep-1L labeled with [²²⁵Ac] (1 µCi (0.04 MBq); intracranial infusion via convection-enhanced delivery; single dose) TFA is well-tolerated and provides significant anti-glioblastoma efficacy, as evidenced by a median survival of 41 days, reduced tumor volume, and induction of tumor cell death and reduced proliferation in orthotopic U251 glioblastoma-bearing mice^[2].

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

2124.47 (free base)

C₈₈H₁₄₆N₂₈O₂₇S₃.xC₂HF₃O₂

Solid

White to off-white

Ala-Cys-Gly-Glu-Met-Gly-Trp-Val-Arg-Cys-Gly-Gly-Gly-Ser-{Ahx}-Lys-Lys(DOTA)-NH2

ACGEMGWVRCGGGS-{Ahx}-K-Lys(DOTA)-NH2

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]. Phipps MD, et al. Current State of Targeted Radiometal-Based Constructs for the Detection and Treatment of Disease in the Brain. Bioconjug Chem. 2021;32(7):1331-1347.

  [2]. Sattiraju A, et al. IL13RA2 targeted alpha particle therapy against glioblastomas. Oncotarget. 2017;8(26):42997-43007.  [Content Brief]