NCS-MP-NODA
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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- No. CAS: 1374994-81-6
- Fòrmula: C18H24N4O4S
- Peso molecular:392.47
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
RDC Bifunctional Chelator |
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. Further protocols information, click here.
In Vivo
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.
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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]
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Dosage:[18F]DK222: ~200 μCi (7.4 MBq); blocking dose of DK221: 50 mg/kg
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Administration:i.v.; single dose; blocking dose given 30 min prior to [18F]DK222 injection
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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.
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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]
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Dosage:~200 μCi (7.4 MBq)
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Administration:i.v.; single dose
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Result:Showed 88% (P < 0.0001) less uptake in SUM149 tumors (low PD-L1 expression) compared to MDAMB231 tumors at 60 min.
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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]
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Dosage:[18F]DK222: ~200 μCi (7.4 MBq); blocking dose of DK221: dose not specified
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Administration:i.v.; single dose; blocking dose given prior to [18F]DK222 injection
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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.
Chemical Information
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No. CAS 1374994-81-6
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Peso molecular 392.47
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Fòrmula C18H24N4O4S
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SMILES
O=C(CN1CCN(CCN(CC1)CC2=CC=C(C=C2)N=C=S)CC(O)=O)O
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Synonyms
NODA-Bz-SCN
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NCS-MP-NODA Related Classifications
HY-164576 Related Classifications
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Keywords
- NCS-MP-NODA
- 1374994-81-6
- NODA-Bz-SCN
- Radionuclide-Drug Conjugates (RDCs)
- colon cancer
- LOX-IMVI melanoma xenografts
- PD-L1
- A375 melanoma xenografts
- triple-negative breast cancer
- melanoma
- MDAMB231 breast cancer xenografts
- MC38-hPD-L1 colon tumor xenografts
- MeWo melanoma xenografts
- SUM149 breast cancer xenografts
- Inhibitor
- inhibitor
- inhibit