1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Antibody-Drug Conjugate/ADC Related
  2. ROR Radionuclide-Drug Conjugates (RDCs)
  3. NP1

NP1 is a NOTA-chelated linear precursor based on the ROR1-targeting peptide. After labeling with [18F]AlF, NP1 yields [18F]AlF-NP1, a PET imaging probe with excellent ROR1 specificity (KD = 141.7 nM), rapid tumor uptake and high target-to-background ratio, which is suitable for non-invasive visualization of various ROR1-overexpressing tumors.

For research use only. We do not sell to patients.

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NP1

NP1 Chemical Structure

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Description

NP1 is a NOTA-chelated linear precursor based on the ROR1-targeting peptide. After labeling with [18F]AlF, NP1 yields [18F]AlF-NP1, a PET imaging probe with excellent ROR1 specificity (KD = 141.7 nM), rapid tumor uptake and high target-to-background ratio, which is suitable for non-invasive visualization of various ROR1-overexpressing tumors[1].

IC50 & Target[1]

ROR-α

141.7 nM (Kd)

In Vitro

[18F]AlF-NP1 (3.125-400 nM; 10-60 min) exhibits specific and high uptake in ROR1-positive MC38 cells, with a KD value of 141.7 nM. It also shows evident uptake in B16F10, A549 and HepG2 cells, and the uptake level in MC38 cells is significantly higher than that in B16F10 cells[1].

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

In Vivo

[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits detectable tumor uptake and target-to-nontarget ratios in HepG2 hepatocellular carcinoma xenograft mice[1].
[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits measurable tumor uptake and target-to-nontarget ratios in A549 lung cancer xenograft mice[1].
[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits high specific tumor uptake and desirable target-to-nontarget ratios in MC38 colon cancer xenograft mice, and is cleared via the kidneys[1].
[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits specific, measurable tumor uptake and target-to-nontarget ratios in B16F10 melanoma allograft mice[1].
[18F]AlF-NP1 (7.4 MBq; intravenous injection; single administration) exhibits renal clearance properties in healthy C57BL/6 mice, with extremely low uptake in other normal tissues[1].

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

Animal Model: BALB/c nude (male, 6-8 weeks old, subcutaneous xenograft via HepG2 cell injection)[1]
Dosage: 3.7 MBq
Administration: i.v.; single dose
Result: Reached ~0.6% ID/g tumor uptake at 30 minutes postinjection.
Achieved ~4 tumor-to-muscle ratio at 30 minutes postinjection.
Achieved ~0.1 tumor-to-kidney ratio at 30 minutes postinjection.
Animal Model: BALB/c nude (male, 6-8 weeks old, subcutaneous xenograft via A549 cell injection)[1]
Dosage: 3.7 MBq
Administration: i.v.; single dose
Result: Reached ~0.5% ID/g tumor uptake at 30 minutes postinjection.
Achieved ~5 tumor-to-muscle ratio at 30 minutes postinjection.
Achieved ~0.05 tumor-to-kidney ratio at 30 minutes postinjection.
Animal Model: C57BL/6 (male, 6-8 weeks old, subcutaneous allograft via MC38 cell injection)[1]
Dosage: 3.7 MBq; 3.7 MBq plus 100 μg/mouse PR7 (blocking studies)
Administration: i.v.; single dose
Result: Reached 2.89% ID/g tumor uptake at 30 minutes postinjection.
Reached 1.32% ID/g tumor uptake at 60 minutes postinjection.
Achieved 2.62 tumor-to-muscle ratio at 60 minutes postinjection.
Reached 27.27% ID/g renal uptake at 30 minutes postinjection.
Reached 17.74% ID/g renal uptake at 60 minutes postinjection.
Reduced tumor uptake significantly when blocked with PR7.
Animal Model: C57BL/6 (male, 6-8 weeks old, subcutaneous allograft via B16F10 cell injection)[1]
Dosage: 3.7 MBq; 3.7 MBq plus 100 μg/mouse PR7 (blocking studies)
Administration: i.v.; single dose
Result: Reached ~0.6% ID/g tumor uptake at 30 minutes postinjection.
Achieved ~3 tumor-to-muscle ratio at 30 minutes postinjection.
Achieved ~0.05 tumor-to-kidney ratio at 30 minutes postinjection.
Reduced tumor uptake significantly when blocked with PR7.
Animal Model: C57BL/6 (male, 6-8 weeks old, normal healthy)[1]
Dosage: 7.4 MBq
Administration: i.v.; single dose
Result: Showed high accumulation in kidneys at 30 and 60 minutes postinjection.
Exhibited extremely low radioactivity in all other organs at 30 and 60 minutes postinjection.
Molecular Weight

2165.25

Formula

C96H132TN26O32

Sequence

NOTA-Ser-Asp-Ile-Asn-Asp-Arg-Gln-Ile-Pro-Gly-Tyr-Ser-Thr-Tyr-Trp-Gly-Asp-Phe-NH2

Sequence Shortening

NOTA-SDINDRQIPGYSTYWGDF-NH2

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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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.

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NP1
Cat. No.:
HY-P11859
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