2. Immunology/Inflammation
  3. CD38
  4. 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.

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

NOTA-MK0159

NOTA-MK0159 Chemical Structure

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NOTA-MK0159 Related Antibodies

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Description

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[1].

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.

NOTA-MK0159 Related Antibodies
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-Prkdcem26Cd52Il2rgem26Cd22/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).
Molecular Weight

753.91

Formula

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
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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NOTA-MK0159 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:

NOTA-MK0159CD38H929 human multiple myeloma cellsU266 human multiple myeloma cellsall-trans retinoic acidmultiple myeloma xenograftsMM.1S human multiple myeloma cellshydrolase enzymatic activitymultiple myeloma cellsdaratumumabwild-type human CD38 proteinInhibitorinhibitorinhibit

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