MRS8288
MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC50 of 0.96 μM against ABCG2 and an IC50 of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research.
For research use only. We do not sell to patients.
- Formula: C36H28ClF2N9O3
- Molecular Weight:708.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
MRS8288 (20 min) potently inhibits the basal ATPase activity of P-glycoprotein derived from High-Five insect cells, with an IC50 of 1.39±0.20 μM[1].
MRS8288 (20 min) potently inhibits the basal ATPase activity of ABCG2 derived from High-Five insect cells, with an IC50 of 0.96±0.15 μM[1].
MRS8288 (0-10 μM) potently inhibits ABCG2-mediated transport of Mitoxantrone (HY-13502) and Pheophorbide A (HY-125665) in HEK293-R5 cells, with IC50 values of 2.49±0.16 μM and 4.86±0.4 μM, respectively[1].
MRS8288 (72 h) exhibits cytotoxicity against both HEK293-pcDNA control cells and HEK293-R5 cells expressing ABCG2, with IC50 values of 5.19±0.1 μM and 4.06±0.6 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 708.12
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Formula C36H28ClF2N9O3
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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(NCC5=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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)