DOTA-Pep-1L TFA
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 98.60%
- Formula: C88H146N28O27S3.xC2HF3O2
- Molecular Weight:2124.47 (free base)
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
IL13 |
In Vivo
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.
Chemical Information
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Appearance Solid
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Molecular Weight 2124.47 (free base)
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Formula C88H146N28O27S3.xC2HF3O2
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Color White to off-white
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Sequence
Ala-Cys-Gly-Glu-Met-Gly-Trp-Val-Arg-Cys-Gly-Gly-Gly-Ser-{Ahx}-Lys-Lys(DOTA)-NH2
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Sequence Shortening
ACGEMGWVRCGGGS-{Ahx}-K-Lys(DOTA)-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Protocols
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Sattiraju A, et al. IL13RA2 targeted alpha particle therapy against glioblastomas. Oncotarget. 2017;8(26):42997-43007. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)