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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- Formule: C35H26ClF2N9O3
- Masse moléculaire:694.09
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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Cell Line:HEK293-pcDNA control cells, ABCG2-expressing HEK293-R5 cells
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Concentration:Up to 50 μM
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Incubation Time:72 h
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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
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Masse moléculaire 694.09
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Formule C35H26ClF2N9O3
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRS8432 Related Classifications
HY-181803 Related Classifications
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