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Referencia número: HY-181803

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MRS8432

MRS8432 is an ABCG2 modulator with an EC₅₀ of 7.5 nM against human ABCG2. MRS8432 activates ABCG2 ATPase activity. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance.

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Fòrmula: C₃₅H₂₆ClF₂N₉O₃
Peso molecular:694.09

Almacenamiento:

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

MRS8432 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- In Vitro
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

In Vitro

MRS8432 (0.1-10 μM; 20 min at 37°C) potently stimulates ABCG2 ATPase activity in High-Five insect cell membranes with an EC₅₀ of 7.5 nM^[1].
MRS8432 (10 μM) partially inhibits ABCG2-mediated efflux of mitoxantrone and pheophorbide A in HEK293-R5 cells when tested at 10 μM^[1].
MRS8432 (up to 50 μM; 72 h) shows low cytotoxicity (IC₅₀ >25 μM) in HEK293-pcDNA and ABCG2-expressing HEK293-R5 cells and is not a substrate for ABCG2-mediated efflux^[1].
MRS8432 binds to the ABCG2 drug-binding pocket in a self-folded conformation that does not engage residue T402, consistent with its stimulatory effect on ABCG2 ATPase activity^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

HEK293-pcDNA control cells, ABCG2-expressing HEK293-R5 cells
Concentration:

Up to 50 μM
Incubation Time:

72 h
Result:

Exhibited IC₅₀ values for cytotoxicity >25 μM in both HEK293-pcDNA and HEK293-R5 cells.
Showed overlapping viability curves indicating MRS8432 is not transported by ABCG2.

Chemical Information

Peso molecular 694.09
Fòrmula C₃₅H₂₆ClF₂N₉O₃
SMILES

O[C@@H]1[C@H](O)[C@](C(NC)=O)(C2)[C@H]2[C@H]1N(C=N3)C4=C3C(NC5=CC=CC(N6N=NC(C7=CC=C(C=C7)Cl)=C6)=C5)=NC(C#CC8=CC=C(C(F)=C8)F)=N4
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Murakami M, et al. (N)-Methanocarba Adenosine Derivatives as Dual Modulators of P-Glycoprotein and ABCG2 Transporters. J Med Chem. 2026;69(4):4945-4968. [Content Brief]

Calculators

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Calculadora de dilución

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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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100 mg

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