P-gp/BCRP-IN-3
P-gp/BCRP-IN-3 is a dual-target inhibitor that acts on P-gp (ABCB1) and BCRP (ABCG2) transporters. P-gp/BCRP-IN-3 directly binds to both transporters, blocks efflux function without affecting protein expression, and restores intracellular accumulation of chemotherapeutic substrates. P-gp/BCRP-IN-3 enhances tumor accumulation and antitumor activity of Mitoxantrone (HY-13502) in colorectal cancer xenograft models. P-gp/BCRP-IN-3 is applicable for cancer-related research.
For research use only. We do not sell to patients.
- Formula: C44H37FN6O4
- Molecular Weight:732.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
P-gp/BCRP-IN-3 (1-10 μM; 4 h) restores intracellular substrate accumulation in MCF-7/ADR and HCT116/ABCG2 cells by directly binding to P-gp/BCRP[1].
P-gp/BCRP-IN-3 (5 μM; 12 h) sensitizes drug-resistant cancer cells in MCF-7/ADR and HCT116/ABCG2 cells without broadly altering stress response pathways, and its reversal effect is achieved through functional inhibition rather than transcriptional perturbation[1].
P-gp/BCRP-IN-3 (1-5 μM; 30 min) directly binds to P-gp and BCRP, forming stable ligand-protein complexes, thereby inhibiting the function of efflux transporters in MCF-7/ADR and HCT116/ABCG2 cells[1].
P-gp/BCRP-IN-3 forms a stable dual binding with P-gp and BCRP, adopting an L-shaped conformation in both transporters[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7/ADR and HCT116/ABCG2
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Concentration:5 μM
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Incubation Time:48 h
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Result:Exhibited a reversal fold against BCRP (RF_BCRP) of 2664.2.
Retained P-gp inhibitory activity (RF_P-gp) of 87.8.
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Cell Line:MCF-7/ADR and HCT116/ABCG2
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Concentration:1, 5, 10 μM
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Incubation Time:48 h
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Result:Did not produce substantial changes in P-gp or BCRP protein levels relative to the control group.
Variations in expression at 10 μM remained below 5%.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 4 weeks old, inoculated with HCT116/ABCG2 cells (5 × 107 cells/0.2 mL)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 2 days; 14 days
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Result:Inhibited tumor growth in combination with Mitoxantrone, with a significant reduction in tumor volume over seven doses.
Did not affect general condition or cause obvious toxicity at 10 mg/kg, with body weight gain slightly greater than control.
Showed organ morphology, organ indices, and hematological parameters comparable to control.
Showed normal tissue morphology in all organs with no additional damage in combination.
Increased mitoxantrone accumulation in tumor tissue by approximately 1.3-fold and reduced mitoxantrone levels in normal tissues by 5% to 21%.
Chemical Information
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Molecular Weight 732.80
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Formula C44H37FN6O4
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SMILES
CC(C=C1)=C(NC2=NC=CC(C3=CC=C(F)C=C3)=N2)C=C1C(NC(C=C4)=CC=C4C(C=C5)=CC6=C5NC(C(N(CC7)CC8=C7C=C(OC)C(OC)=C8)=O)=C6)=O
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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)
P-gp/BCRP-IN-3 Related Classifications
HY-189363 Related Classifications
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