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^[1].

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.

694.09

C₃₅H₂₆ClF₂N₉O₃

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

Room temperature in continental US; may vary elsewhere.

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

• [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]