NYM074
NYM074 is a carbonic anhydrase IX (CAIX) ligand. NYM074 binds specifically to human CAIX to enable targeted radionuclide delivery. NYM074 supports dual radiolabeling with 68Ga for positron emission tomography (PET) imaging and 177Lu for radionuclide applications. NYM074 can be used for the research of clear cell renal cell carcinoma.
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- Fòrmula: C41H59N11O12S2
- Peso molecular:962.10
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
hCA IX |
In Vitro
NYM074 (0.5-500 nM; 240 s) binds with high, selective affinity to recombinant human CAIX (Kd = 0.65 nM) compared to human CAII and CAXII in an in vitro SPR assay[1].
NYM074, when radiolabeled as [68Ga]Ga-NYM074, is selectively taken up by CAIX-positive OS-RC-2 cells in an in vitro assay, with uptake significantly reduced by 100-fold excess unlabeled NYM074, while CAIX-negative PC-3 cells show minimal uptake[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | V | CL | MRT0-t | MRT0-inf | Vss |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 28.57 μg/kg | i.v. | 3.3 h | 0.02 h | 2.54 L/kg | 0.53 L/h/kg | 1.32 h | 5.03 h | 2.69 L/kg |
In Vivo
NYM074 (0.1 mCi; i.v.; single dose) achieves peak tumor uptake of 9.57 %ID/g at 60 minutes in OS-RC-2 ccRCC xenograft mice following radiolabelled with 68Ga[1].
NYM074 (0.3 mCi; i.v.; single dose) exhibits high and prolonged tumor uptake of 29.15 %ID/g at 4 hours in OS-RC-2 ccRCC xenograft mice following radiolabelled with 177Lu, with a calculated tumor absorbed dose of 296 mGy/MBq[1].
NYM074 (28.57 μg/kg; i.v.; single dose) exhibits a half-life of 3.3 hours and predominant renal excretion in healthy ICR mice following radiolabelled with 68Ga, with highest uptake in kidneys and liver[1].
NYM074 (2 mCi; i.v.; single dose; 14 days) does not induce notable histopathological changes in major organs of healthy ICR mice following radiolabelled with 177Lu[1].
NYM074 (0.3 mCi; i.v.; single dose) exhibits predominant renal excretion with highest uptake in kidneys and liver in healthy ICR mice following radiolabelled with 177Lu, with minimal bone uptake indicating in vivo stability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 6-8 weeks, 18-22 g, subcutaneously inoculated with OS-RC-2 tumor cells)[1]
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Dosage:2 mCi
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Administration:i.v.; single dose or two doses with 7-day interval; up to 30 days
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Result:Resulted in a final tumor volume of 1248.89 mm3, a T/C ratio of 65.24%, and a tumor growth inhibition (TGI) of 40.47% compared to the saline control group.
Resulted in a final tumor volume of 547.55 mm3, a T/C ratio of 25.33%, and a TGI of 73.90% (P < 0.001 vs. saline).
Showed stable body weights with <5% loss, with no significant difference from the vehicle control group.
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Animal Model:BALB/c nude mice (female, 6-8 weeks, 18-22 g, subcutaneously inoculated with OS-RC-2 tumor cells)[1]
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Dosage:0.1 mCi
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Administration:i.v.; single dose
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Result:Showed time-dependent tumor uptake, peaking at 9.57 %ID/g at 60 minutes post-injection.
Reached a tumor-to-muscle ratio of 8.25 at 60 minutes.
Reduced tumor uptake by 78.69% with co-injection of 10 mg/kg acetazolamide, confirming specific CAIX targeting.
Decreased renal uptake over time from 19.85 %ID/g at 10 minutes to 13.74 %ID/g at 120 minutes.
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Animal Model:BALB/c nude mice (female, 6-8 weeks, 18-22 g, subcutaneously inoculated with OS-RC-2 tumor cells)[1]
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Dosage:0.3 mCi
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Administration:i.v.; single dose
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Result:Showed sustained tumor retention, with ex vivo uptake of 29.15 %ID/g at 4 hours and 3.28 %ID/g at 48 hours post-injection.
Achieved a calculated tumor absorbed dose of 296 mGy/MBq.
Declined liver and kidney radioactivity significantly over time.
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Animal Model:ICR mice (6-week-old)[1]
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Dosage:28.57 μg/kg
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Administration:i.v.; single dose
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Result:Showed highest uptake in kidneys (11.31 %ID/g at 15 minutes; 13.97 %ID/g at 60 minutes; 13.05 %ID/g at 120 minutes; 11.04 %ID/g at 240 minutes) and liver (9.63 %ID/g at 15 minutes; 9.70 %ID/g at 60 minutes; 9.76 %ID/g at 120 minutes; 8.47 %ID/g at 240 minutes).
Achieved a half-life (T1/2) of 3.3 hours, moderate clearance rate (CL_obs = 0.53 (L/h)/kg), and mean residence time (MRT(0-inf)_obs) of 5.03 hours.
Reached effective absorbed doses for male/female mice of 0.012/0.015 mSv/MBq.
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Animal Model:ICR mice (healthy adult, 20-25 g, half male/half female)[1]
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Dosage:2 mCi
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Administration:i.v.; single dose; 14 days
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Result:Revealed intact tissue architecture and normal cellular morphology in kidneys, liver, spleen, lungs, and heart.
Showed no significant inflammation, necrosis, fibrosis, hemorrhage, or other treatment-related pathological alterations.
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Animal Model:ICR mice[1]
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Dosage:0.3 mCi
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Administration:i.v.; single dose
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Result:Showed highest uptake in kidneys (52.78 %ID/g at 1 hour; 34.36 %ID/g at 6 hours; 5.67 %ID/g at 24 hours; 4.64 %ID/g at 48 hours) and liver (34.25 %ID/g at 1 hour; 28.53 %ID/g at 6 hours; 1.93 %ID/g at 24 hours; 0.47 %ID/g at 48 hours).
Showed uptake in brain, spleen, bone, and bone marrow of <0.25 %ID/g at all time points.
Reached whole-body effective doses for male/female mice of 0.026/0.035 mSv/MBq.
Chemical Information
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Peso molecular 962.10
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Fòrmula C41H59N11O12S2
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SMILES
O=C(CCCCC(N[C@@H](CC1=CC(C=CC=C2)=C2C=C1)C(NCCCCNC(CN3CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC3)=O)=O)=O)NC4=NN=C(S(=O)(N)=O)S4
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NYM074 Related Classifications
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