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United States

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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₃₆H₅₁N₉O₇S
分子量:753.91

保管条件:

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

NOTA-MK0159 構造式

容量

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数量

Amount: USD 0.00

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

生物活性

製品説明

体外実験

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.

体内実験

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).

化学情報

分子量 753.91
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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]

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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

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100 mg

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