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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C36H51N9O7S
- Peso molecular:753.91
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG (NOD/ShiLtJGpt-Prkdcem26Cd52Il2rgem26Cd22/Gpt) (subcutaneous multiple myeloma xenograft via right hindlimb injection of 5×106 U266 cells)[1]
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Dosage:5.55-7.4 MBq
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Administration:i.v.; single dose via tail vein; two separate administrations
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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
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Peso molecular 753.91
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Fòrmula C36H51N9O7S
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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
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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)
NOTA-MK0159 Related Classifications
HY-182345 Related Classifications
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