NSC 23925B
NSC 23925B is a P-glycoprotein (P-gp) inhibitor, as well as the most biologically active isomer of NSC23925 (HY-19626), which reverses and prevents P-glycoprotein-mediated multidrug resistance in cancer cells. NSC 23925B shows weak inhibition against most CYP450 enzymes (IC50 > 10 μM), and exhibits moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B can be used for the research of multidrug-resistant cancers.
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- CAS No.: 1369591-04-7
- Formule: C22H26Cl2N2O2
- Masse moléculaire:421.36
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
In Vitro
NSC 23925B potently reverses Pgp-mediated multidrug resistance (MDR) in multidrug-resistant human breast cancer and colon cancer cell lines[1].
NSC 23925B inhibits Pgp-mediated chemoresistance in ovarian cancer cells and osteosarcoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NSC 23925B (2.50-47.20 mg/kg; i.p.; i.v.; single dose) exhibits favorable pharmacokinetic profiles with high bioavailability, measurable plasma concentrations over 24 hours, and limited toxicity in male Sprague-Dawley rats, with a maximum tolerated dose of at least 33.10 mg/kg (i.p.) and 38.80 mg/kg (i.v.) in males[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1369591-04-7
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Masse moléculaire 421.36
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Formule C22H26Cl2N2O2
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SMILES
O[C@H]([C@@]1([H])CCCCN1)C2=CC(C3=CC=C(C=C3)OC)=NC4=C2C=CC=C4.Cl.Cl
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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)
Keywords
- NSC 23925B
- 1369591-04-7
- P-glycoprotein
- Cytochrome P450
- Drug Isomer
- P-gp
- Pgp
- Multidrug resistance protein 1
- MDR1
- ATP-binding cassette sub-family B member 1
- ABCB1
- Cluster of differentiation 243
- CD243
- CYPs
- CYP2B6
- CYP3A4
- CYP1A2
- Sprague-Dawley rats
- cancer cells
- CYP2D6
- multidrug resistance
- BALB/c mice
- cytochrome P450
- Inhibitor
- inhibitor
- inhibit