2. Antibody-drug Conjugate/ADC Related
  3. Radionuclide-Drug Conjugates (RDCs)
  4. 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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NCS-MP-NODA

NCS-MP-NODA Chemical Structure

CAS No. : 1374994-81-6

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NCS-MP-NODA Related Antibodies

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Description

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[1][2][3].

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.

NCS-MP-NODA Related Antibodies
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.
Molecular Weight

392.47

Formula

C18H24N4O4S
CAS No.
SMILES

O=C(CN1CCN(CCN(CC1)CC2=CC=C(C=C2)N=C=S)CC(O)=O)O
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
References
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NCS-MP-NODA Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

NCS-MP-NODA1374994-81-6NODA-Bz-SCNRadionuclide-Drug Conjugates (RDCs)colon cancerLOX-IMVI melanoma xenograftsPD-L1A375 melanoma xenograftstriple-negative breast cancermelanomaMDAMB231 breast cancer xenograftsMC38-hPD-L1 colon tumor xenograftsMeWo melanoma xenograftsSUM149 breast cancer xenograftsInhibitorinhibitorinhibit

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