ABCB1-IN-3
ABCB1-IN-3 (Compound K27) is an orally active inhibitor of ABCB1, and induces apoptosis. ABCB1-IN-3 directly binds to ABCB1 to inhibit efflux function, ensuring stable intracellular concentration of Paclitaxel (PTX) (HY-B0015) without affecting ABCB1 normal expression. ABCB1-IN-3 significantly increases the sensitivity of ABCB1-mediated multidrug resistance (MDR) to Paclitaxel in vitro, enhances cell cycle arrest, and inhibits proliferation. BCB1-IN-3 combined with Paclitaxel exhibits potent tumor suppression in vivo without generating toxicity.
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- 화학식: C19H16N2O
- 분자량:288.34
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
ABCB1-IN-3 (72 h) significantly increases the sensitivity of ABCB1-mediated MDR SW620/AD300 cells to Paclitaxel (IC50 = 15.33 nM) and hardly shows toxicity even at a high concentration of 20 μM when used alone[1].
ABCB1-IN-3 (5-20 μM; 24 h) distinctly enhances the arresting effect of Paclitaxel on the SW620/AD300 cell cycle, thereby inhibiting their proliferation[1].
ABCB1-IN-3 (5-20 μM; 7 d) combined with Paclitaxel inhibits the cell colony formation, exhibits great reversal activity against Paclitaxel resistance cells[1].
ABCB1-IN-3 (5-20 μM; 24 h) is confirmed to directly bind to ABCB1 to inhibit efflux function, reducing cellular efflux and ensuring stable intracellular concentration of Paclitaxel without affecting ABCB1 normal expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620/AD300 cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 h
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Result:Induced more cells to stay in the G2/M phase combined with Paclitaxel.
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Cell Line:SW620/AD300 cells
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Concentration:5, 10, 20 μM
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Incubation Time:7 days
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Result:Significantly inhibited the cell colony formation of SW620/AD300 cells combined with Paclitaxel.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice (18-22 g, aged 6-7 weeks, 1×107 SW620/AD300 cells were inoculated subcutaneously into the forelimb of each mouse.)[1]
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Dosage:50 mg/kg
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Administration:Intragastric gavage (i.g.); once every 3 days for 14 days
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Result:The tumor volume and weight had little difference when used alone, and remarkable reduced when combined with Paclitaxel, showing better antitumor activity.
The cell apoptosis in tumor tissues was more remarkable when used with Paclitaxel, resulted in more massive degeneration and necrosis than in vehicle or mono-therapy groups.
Showed no significant loss of body weight.
Chemical Information
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분자량 288.34
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화학식 C19H16N2O
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SMILES
CN1C2=CC=CC=C2C3=C1C(C4=CC=C(OC)C=C4)=NC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ABCB1-IN-3 Related Classifications
HY-168921 Related Classifications
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