P-gp inhibitor 21
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity.
For research use only. We do not sell to patients.
- Formula: C27H42N2O4
- Molecular Weight:458.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI/ADR-RES | IC50 |
27.9 nM
Compound: 56
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Reversal effect on P-gp-mediated multidrug resistance in human NCI/ADR-RES cells assessed as inhibition of cell proliferation by measuring VNR IC50 at 10 uM incubated for 72 hrs in presence of VNR by SRB assay
Reversal effect on P-gp-mediated multidrug resistance in human NCI/ADR-RES cells assessed as inhibition of cell proliferation by measuring VNR IC50 at 10 uM incubated for 72 hrs in presence of VNR by SRB assay
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[PMID: 38502936] |
| NCI/ADR-RES | IC50 |
56.9 nM
Compound: 56
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Reversal effect on P-gp-mediated multidrug resistance in human NCI/ADR-RES cells assessed as inhibition of cell proliferation by measuring PTX IC50 at 10 uM incubated for 72 hrs in presence of PTX by SRB assay
Reversal effect on P-gp-mediated multidrug resistance in human NCI/ADR-RES cells assessed as inhibition of cell proliferation by measuring PTX IC50 at 10 uM incubated for 72 hrs in presence of PTX by SRB assay
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[PMID: 38502936] |
| NCI/ADR-RES | IC50 |
767.3 nM
Compound: 56
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Reversal effect on P-gp-mediated multidrug resistance in human NCI/ADR-RES cells assessed as inhibition of cell proliferation by measuring ADR IC50 at 10 uM incubated for 72 hrs in presence of ADR by SRB assay
Reversal effect on P-gp-mediated multidrug resistance in human NCI/ADR-RES cells assessed as inhibition of cell proliferation by measuring ADR IC50 at 10 uM incubated for 72 hrs in presence of ADR by SRB assay
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[PMID: 38502936] |
P-gp inhibitor 21 inhibits proliferations of cells KBV200 and NCI/ADR-RES (combined with VNR) with IC50s of 2.4 and 27.9 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis of P-gp inhibitor 21 in mice[1]
| route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUClast (ng·h/mL) | AUCinf_obs (ng·h/mL) | CLobs (mL/min/kg) | MRTinf_obs (h) | Vss (mL/kg) | F (%) |
| iv | 1 | - | - | 1260 | 1263 | 33.5 | 0.75 | 1528 | - | |
| po | 30 | 0.25 | 34.4 | 32.3 | 43.4 | - | 3.11 | - | 0.09 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KBV200 xenograft BALB/c nude mice[1]
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Dosage:75 mg/kg
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Administration:i.p.
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Result:Suppressed tumor growth without significant body weight loss.
Chemical Information
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Molecular Weight 458.63
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Formula C27H42N2O4
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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 inhibitor 21 Related Classifications
HY-162396 Related Classifications
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