1. Antibody-drug Conjugate/ADC Related Neuronal Signaling GPCR/G Protein
  2. Radionuclide-Drug Conjugates (RDCs) Neurotensin Receptor
  3. DOTA-NT-20.3-IPBA

DOTA-NT-20.3-IPBA is a Neurotensin receptor 1 (NTR1)-targeting albumin binder with specific high-affinity binding to NTR1. DOTA-NT-20.3-IPBA is formed by the conjugation of DOTA-NT-20.3 and IPBA. DOTA-NT-20.3-IPBA can be used for positron emission tomography (PET) imaging following labeling with [68Ga]Ga.

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DOTA-NT-20.3-IPBA

DOTA-NT-20.3-IPBA Chemical Structure

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Description

DOTA-NT-20.3-IPBA is a Neurotensin receptor 1 (NTR1)-targeting albumin binder with specific high-affinity binding to NTR1. DOTA-NT-20.3-IPBA is formed by the conjugation of DOTA-NT-20.3 and IPBA. DOTA-NT-20.3-IPBA can be used for positron emission tomography (PET) imaging following labeling with [68Ga]Ga[1].

IC50 & Target[1]

NTR1

 

In Vitro

DOTA-NT-20.3-IPBA binds to human albumin (PDB ID: 5yoq) with a binding energy of −8.1 kcal/mol, forming hydrogen bonds with 10 specific amino acid residues[1].
DOTA-NT-20.3-IPBA binds to human NTR1 (PDB ID: 4grv) with a binding energy of −8.7 kcal/mol, forming hydrogen bonds with 9 specific amino acid residues[1].
DOTA-NT-20.3-IPBA (20 μg; 10 min heated at 95 °C) can be radiolabeled with 68Ga to produce [68Ga]Ga-DOTA-NT-20.3-IPBA with >95% radiochemical yield, >95% radiochemical purity, and a molar activity of 5−6 MBq/nmol[1].
DOTA-NT-20.3-IPBA (~0.74 MBq) has a LogP value of -2.37 following labeling with 68Ga[1].
DOTA-NT-20.3-IPBA (~0.37 MBq; 1 h) binds to mouse serum albumin at a rate of 19.27% following labeling with 68Ga[1].
DOTA-NT-20.3-IPBA (~1.48 MBq; 1-2 h) maintains >95% intactness following labeling with 68Ga after 2 h of in vitro incubation in PBS at room temperature or mouse serum at 37 °C[1].
DOTA-NT-20.3-IPBA (5-100 nM; 1 h) binds to NTR1 on HT-29 cells with a dissociation constant (Kd) of 33.86 nM following labeling with 68Ga[1].
DOTA-NT-20.3-IPBA (~0.15 MBq; 1-3 h) is taken up at significantly higher levels by NTSR1-high expressing HT-29 cells than NTSR1-low expressing SKOV3 cells following labeling with 68Ga, and this uptake is specifically inhibited by excess NT-20.3, demonstrating NTR1-specific binding[1].

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

In Vivo

DOTA-NT-20.3-IPBA (~3.7 MBq; i.v.; single injection) achieves specific, sustained NTR1-targeted tumor uptake in HT-29 xenograft mice following labeling with 68Ga[1].
DOTA-NT-20.3-IPBA (7.4 MBq; i.v.; single injection) exhibits a prolonged systemic circulation half-life of 30.43 minutes in normal mice following labeling with 68Ga[1].
DOTA-NT-20.3-IPBA (~7.4 MBq; i.v.; single injection) causes no detectable organ damage in healthy BALB/c nude mice at 24 hours postinjection following labeling with 68Ga[1].

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

Animal Model: BALB/c nude mice (female, 5−6 weeks old, subcutaneous implantation of 5×106 HT-29 cells)[1]
Dosage: ~3.7 MBq
Administration: i.v.; single injection
Result: Reached tumor uptake of 2.67 % ID/g at 30 min p.i., 2.37 % ID/g at 60 min p.i., and 2.07 % ID/g at 120 min p.i. following labeling with 68Ga.
Animal Model: BALB/c nude mice (female, 6−8 weeks old)[1]
Dosage: 7.4 MBq
Administration: i.v.; single injection
Result: Exhibited an elimination half-life of 30.43 minutes following labeling with 68Ga.
Animal Model: BALB/c nude mice (female, 5−6 weeks old)[1]
Dosage: ~7.4 MBq
Administration: i.v.; single injection
Result: Caused no observable damage to heart, liver, spleen, lung, or kidney, matching the PBS control group following labeling with 68Ga.
Molecular Weight

1712.77

Formula

C76H118IN19O18

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
DOTA-NT-20.3-IPBA
Cat. No.:
HY-P11845
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