Tyr3-Octreotate
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.76%
- CAS No.: 302794-43-0
- Formula: C49H64N10O12S2
- Molecular Weight:1049.22
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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]|
SSTR2 |
RDC Peptide |
In Vitro
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:specific strain not specified[1]
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Dosage:277.5 MBq (small tumors, 2 doses; large tumors, single dose; large tumors, 2 doses); 555 MBq (small tumors, single dose)
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Administration:i.v.; single dose; 2 doses
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Result:Achieved a 40% cure rate in rats with larger tumors treated with a single dose of 277.5 MBq.
Achieved a 50% cure rate in rats with larger tumors treated with two doses of 277.5 MBq.
Chemical Information
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CAS No. 302794-43-0
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Appearance Solid
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Molecular Weight 1049.22
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Formula C49H64N10O12S2
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Color White to off-white
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Sequence
{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Thr-Cys-Thr (Disulfide bridge: Cys2-Cys7)
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Sequence Shortening
{d-Phe}-CY-{d-Trp}-KTCT (Disulfide bridge: Cys2-Cys7)
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (263 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)