2. Metabolic Enzyme/Protease Antibody-drug Conjugate/ADC Related
  3. Carbonic Anhydrase Radionuclide-Drug Conjugates (RDCs)
  4. 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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NYM074

NYM074 Chemical Structure

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NYM074 Related Antibodies

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CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

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Description

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[1].

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.

NYM074 Related Antibodies
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 (2 mCi; i.v.; single dose, two doses with 7-day interval; up to 30 days) achieves a maximum tumor growth inhibition of 73.90% in OS-RC-2 ccRCC xenograft mice with excellent tolerability following radiolabelled with 177Lu[1].
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.

Animal Model: BALB/c nude mice (female, 6-8 weeks, 18-22 g, subcutaneously inoculated with OS-RC-2 tumor cells)[1]
Dosage: 2 mCi
Administration: i.v.; single dose or two doses with 7-day interval; up to 30 days
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.
Animal Model: BALB/c nude mice (female, 6-8 weeks, 18-22 g, subcutaneously inoculated with OS-RC-2 tumor cells)[1]
Dosage: 0.1 mCi
Administration: i.v.; single dose
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.
Animal Model: BALB/c nude mice (female, 6-8 weeks, 18-22 g, subcutaneously inoculated with OS-RC-2 tumor cells)[1]
Dosage: 0.3 mCi
Administration: i.v.; single dose
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.
Animal Model: ICR mice (6-week-old)[1]
Dosage: 28.57 μg/kg
Administration: i.v.; single dose
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.
Animal Model: ICR mice (healthy adult, 20-25 g, half male/half female)[1]
Dosage: 2 mCi
Administration: i.v.; single dose; 14 days
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.
Animal Model: ICR mice[1]
Dosage: 0.3 mCi
Administration: i.v.; single dose
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.
Molecular Weight

962.10

Formula

C41H59N11O12S2
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
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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NYM074 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:

NYM074NYM 074NYM-074Carbonic AnhydraseRadionuclide-Drug Conjugates (RDCs)Carbonate dehydratasexenograft model miceclear cell renal cell carcinomaOS-RC-2 cellsPC-3 cellshuman CAIXhuman CAIIhuman CAXIIradionuclide deliverycarbonic anhydrase IXICR miceInhibitorinhibitorinhibit

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