TATE-DA-I
TATE-DA-I is a somatostatin receptor 2 (SSTR2) ligand with an IC50 of 25.3 nM. TATE-DA-I binds to albumin to prolong its circulation retention time and also exhibits enhanced tumor accumulation capacity. TATE-DA-I enables clear visualization of SSTR2-positive tumors in SPECT/CT imaging. TATE-DA-I can be used in cancer-related research.
For research use only. We do not sell to patients.
- Formula: C87H119IN16O25S2
- Molecular Weight:1980.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
SSTR2 25.3 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AR-42J cell line | IC50 |
25.3 nM
|
Inhibition of [111In]In-DOTA-TATE binding to SSTR2 on AR42J rat pancreatic exocrine adenocarcinoma cells by metal-free TATE-DA-I, assessed via radioactivity measurement after 2 h incubation at 37 °C.
Inhibition of [111In]In-DOTA-TATE binding to SSTR2 on AR42J rat pancreatic exocrine adenocarcinoma cells by metal-free TATE-DA-I, assessed via radioactivity measurement after 2 h incubation at 37 °C.
|
41710742 |
In Vitro
TATE-DA-I inhibits SSTR2 binding on AR42J cells with an IC50 of 25.3 nM, and its potency is significantly lower than that of DOTA-TATE (HY-106244)[1].
TATE-DA-I radiolabeled derivative [111In]In-TATE-DA-I shows high in vitro stability in mouse plasma and human plasma after incubation at 37 °C for 24 h[1].[1].
TATE-DA-I radiolabeled derivative [111In]In-TATE-DA-I specifically binds to somatostatin receptor 2 (SSTR2) on AR42J cells[1].
TATE-DA-I radiolabeled derivative [111In]In-TATE-DA-I displays the highest relative binding activity to human serum albumin among all tested radioligands, and its binding rate rises as HSA concentration increases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
TATE-DA-I radiolabeled derivative [111In]In-TATE-DA-I (37 kBq; single intravenous injection) specifically binds to somatostatin receptor 2 in vivo[1].
TATE-DA-I radiolabeled derivative [111In]In-TATE-DA-I (4.9 MBq; intravenous single injection) achieves clear visualization of SSTR2-positive neuroendocrine tumors by SPECT/CT imaging at 24 h and 48 h after injection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1980.00
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Formula C87H119IN16O25S2
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Sequence
Cyclo(Thr-Cys-Thr-Lys-{d-Trp}-Tyr-Cys)-{d-Phe}-{Tetraxetan(Bi(C2-CO))}-{γ-Lys}-{CO-C3-PhI} (Disulfide bridge:Cys2-Cys7)
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Sequence Shortening
Cyclo(TCTK-{d-Trp}-YC)-{d-Phe}-{Tetraxetan(Bi(C2-CO))}-{γ-Lys}-{CO-C3-PhI} (Disulfide bridge:Cys2-Cys7)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)