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Art. -Nr.: HY-164576

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NCS-MP-NODA

Name: NCS-MP-NODA
Brand: MedChemExpress
SKU: HY-164576
Availability: PreOrder

(Synonyms: NODA-Bz-SCN)

NCS-MP-NODA (NODA-Bz-SCN) is a NODA-derived bifunctional chelator. NCS-MP-NODA can conjugate with biomolecules including the RGD tripeptide, and is used for aluminum-[¹⁸F] fluoride-based positron emission tomography (PET) radiolabeling. NCS-MP-NODA can conjugate with the free lysine amino group of the PD-L1-specific peptide DK221 to generate DK222, which can be radiolabeled with ¹⁸F to form [¹⁸F]DK222. NCS-MP-NODA can be used in studies related to triple-negative breast cancer, melanoma and colon cancer.

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CAS. Nr.: 1374994-81-6
Formel: C₁₈H₂₄N₄O₄S
Molecular Weight:392.47

Speicherung:

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

Data Sheet (275 KB)

NCS-MP-NODA Chemical Structure

CAS. Nr.: 1374994-81-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

RDC Bifunctional Chelator

Alle Radionuclide-Drug Conjugates (RDCs) Isoform-spezifische Produkte anzeigen :

In Vitro

NCS-MP-NODA conjugates to the free lysine amine of DK221 under room temperature conditions to form DK222, a peptide suitable for radiofluorination^[3].

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

In Vivo

The tracer [¹⁸F]DK222 (7.4 MBq; intravenous injection; single dose), synthesized from NCS-MP-NODA, exhibits high tumor uptake and specificity for PD-L1 in MDAMB231 breast cancer xenografts; its tumor uptake decreases by 79% when a blocking dose of DK221 (50 mg/kg; intravenous injection; single dose; administered 30 minutes prior to [¹⁸F]DK222 injection) is given^[3].
The tracer [¹⁸F]DK222 (7.4 MBq; intravenous injection; single dose), synthesized from NCS-MP-NODA, shows extremely low uptake in SUM149 breast cancer xenografts with low PD-L1 expression, which is 88% lower than that in MDAMB231 tumors with high PD-L1 expression^[3].
The tracer [¹⁸F]DK222 (7.4 MBq; intravenous injection; single dose), synthesized from NCS-MP-NODA, exhibits high specific uptake in PD-L1-overexpressing LOX-IMVI melanoma xenografts; its uptake is significantly reduced after administration of a blocking dose of DK221 (intravenous injection; single dose) prior to [¹⁸F]DK222 injection^[3].

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

Animal Model:

NSG (nonobese, diabetic, severe-combined immunodeficient gamma; 5- to 6-wk-old; male or female; orthotopic implantation of 2 × 10^6 MDAMB231 human triple-negative breast cancer cells)^[3]
Dosage:

[18F]DK222: ~200 μCi (7.4 MBq); blocking dose of DK221: 50 mg/kg
Administration:

i.v.; single dose; blocking dose given 30 min prior to [18F]DK222 injection
Result:

Showed high accumulation in MDAMB231 tumors as early as 15 min, with tumor uptake remaining consistently high for 4 h after injection.
Reached a tumor-to-blood ratio of 4.5 and tumor-to-muscle ratio of 30.0 at 60 min.
Reduced tumor uptake by 79% (P < 0.0001) in mice receiving the blocking dose of DK221.

Animal Model:

NSG (nonobese, diabetic, severe-combined immunodeficient gamma; 5- to 6-wk-old; male or female; orthotopic implantation of 5 × 10^6 SUM149 human triple-negative breast cancer cells)^[3]
Dosage:

~200 μCi (7.4 MBq)
Administration:

i.v.; single dose
Result:

Showed 88% (P < 0.0001) less uptake in SUM149 tumors (low PD-L1 expression) compared to MDAMB231 tumors at 60 min.

Animal Model:

NSG (nonobese, diabetic, severe-combined immunodeficient gamma; 5- to 6-wk-old; male or female; intradermal implantation of 5 × 10^6 LOX-IMVI human melanoma cells)^[3]
Dosage:

[18F]DK222: ~200 μCi (7.4 MBq); blocking dose of DK221: dose not specified
Administration:

i.v.; single dose; blocking dose given prior to [18F]DK222 injection
Result:

Showed high accumulation of radioactivity in LOX-IMVI tumors in imaging and biodistribution studies.
Showed significantly reduced tumor uptake in mice receiving the blocking dose of DK221.

Related Protocols :

Breast Cancer Modeling

Chemical Information

CAS. Nr. 1374994-81-6
Molecular Weight 392.47
Formel C₁₈H₂₄N₄O₄S
SMILES

O=C(CN1CCN(CCN(CC1)CC2=CC=C(C=C2)N=C=S)CC(O)=O)O
Synonyms

NODA-Bz-SCN
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. San C, et al. Optimization study of a NODA derivative radiofluorination by Al18F complexation using a design of experiments approach[J]. Chemistry-A European Journal, 2023.

[2]. San C, et al. Optimization of a 1,4,7-Triazacyclononane-1,4-diacetic acid (NODA) Derivative Radiofluorination by Al F Complexation Using a Design of Experiments Approach. Chemistry (Weinheim an der Bergstrasse, Germany). 2023 Dec 19;29(71):e202302745. [Content Brief]

[3]. Kumar D, et al. Pharmacodynamic measures within tumors expose differential activity of PD(L)-1 antibody therapeutics. Proc Natl Acad Sci U S A. 2021 Sep 14;118(37):e2107982118. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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