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Cat. No.: HY-182345

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NOTA-MK0159

NOTA-MK0159 is a NOTA (HY-134418) and MK0159 (HY-150508) conjugate. NOTA-MK0159 inhibits human and mouse CD38 with IC₅₀ values of 72.58 and 7.55 nM. NOTA-MK0159 coupled with radioactive elements acts as a imaging agent with specific uptake in CD38-positive multiple myeloma cells, enabling noninvasive whole-body assessment of CD38 expression in multiple myeloma xenografts. NOTA-MK0159 can be used for the research of multiple myeloma.

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화학식: C₃₆H₅₁N₉O₇S
분자량:753.91

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

NOTA-MK0159 Chemical Structure

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Amount: USD 0.00

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Antibody-Drug Conjugates

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Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

In Vitro

NOTA-MK0159 binds to the extracellular domain of wild-type human CD38 protein with a binding free energy score of -7.255 kcal/mol^[1].
NOTA-MK0159 inhibits human CD38 hydrolase activity with an IC₅₀ of 72.58 nM and mouse CD38 hydrolase activity with an IC₅₀ of 7.55 nM^[1].
NOTA-MK0159 (⁶⁸Ga-NOTA-MK0159) (1 μCi; 60 min) exhibits specific CD38-dependent uptake in H929 human multiple myeloma cells^[1].

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

In Vivo

NOTA-MK0159 (⁶⁸Ga-NOTA-MK0159) (5.55-7.4 MBq; i.v.; single dose via tail vein; two separate administrations) can noninvasively detect increased CD38 expression in U266 multiple myeloma xenografts following ATRA (HY-14649) treatment, with significant increases in tumor uptake and tumor-to-muscle ratio^[1].

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

Animal Model:

NCG (NOD/ShiLtJGpt-Prkdc^em26Cd52Il2rg^em26Cd22/Gpt) (subcutaneous multiple myeloma xenograft via right hindlimb injection of 5×10⁶ U266 cells)^[1]
Dosage:

5.55-7.4 MBq
Administration:

i.v.; single dose via tail vein; two separate administrations
Result:

Increased tumor uptake from 0.67 %ID/g to 1.80 %ID/g after 3 days of ATRA treatment (p = 0.007).
Increased tumor-to-muscle ratio from 1.06 to 3.57 after 3 days of ATRA treatment (p = 0.002).

Chemical Information

분자량 753.91
화학식 C₃₆H₅₁N₉O₇S
SMILES

O=C(N1CCN(CC1)CCCO[C@@H]2CC[C@@H](NC(C3=C4C(NC=C4)=NC(C5=CN=CS5)=C3)=O)CC2)CN6CCN(CCN(CC6)CC(O)=O)CC(O)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Duan C, et al. CD38-Targeted Small-Molecule PET Radiotracer for Noninvasive Tumor Evaluation and Preliminary Therapy Monitoring in Multiple Myeloma. J Med Chem. 2026;69(6):7068-7081. [Content Brief]

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

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Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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