P-gp inhibitor 3
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
For research use only. We do not sell to patients.
- CAS No.: 2766451-11-8
- Formula: C48H67N3O6
- Molecular Weight:782.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
P-glycoprotein
P-gp inhibitor 3 (compound 16) (10 μM; 72 hours) has appreciable cytotoxicity in KBV cancer cells, with relatively stronger MDR reversal ability[1].
P-gp inhibitor 3 (2.5, 5, 10 μM ; 3 hours) reverses tumor MDR by inhibiting the efflux function of P-gp[1].
P-gp inhibitor 3 (0.25, 0.5, 1 mM; 5 minutes) can significantly increase ATP consumption in a concentration-dependent manner (p<0.01)[1].
P-gp inhibitor 3 (10 μM; 24 hours) induces apoptosis in KBV cells in the G2/M phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KBV cells[1]
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Concentration:10 μM
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Incubation Time:72 hours
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Result:Showed appreciable cytotoxicity in KBV cancer cells, and exhibited relatively stronger MDR reversal ability.
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Cell Line:KBV cells[1]
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Induced apoptosis in KBV cells in the G2/M phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice xenograft tumor model (6-8 weeks old, BALB/c, male)[1]
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Dosage:10 mg/kg for P-gp inhibitor 3; 30 mg/kg for paclitaxel
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Administration:i.p.; once a day (P-gp inhibitor 3), once every three days (paclitaxel); for 1 to 18 days
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Result:Significantly enhanced the anti-tumor activity of paclitaxel and the tumor suppression rate was 56.24%.
Chemical Information
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CAS No. 2766451-11-8
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Molecular Weight 782.06
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Formula C48H67N3O6
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SMILES
O=C([C@]12[C@](CC(C)(CC2)C)([H])C3=CC[C@@]([C@@]4([C@@]([C@@](C)(C5=C(C=NO5)C4)COC(CCC(N6CCN(CC6)CC)=O)=O)([H])CC7)C)([H])[C@]7(C)[C@@]3(CC1)C)OCC8=CC=CC=C8
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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)