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Art. -Nr.: HY-164585

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P-gp modulator-6

P-gp modulator-6 is a P-glycoprotein (P-gp) modulator. P-gp modulator-6 regulates the substrate specificity of P-gp and enhances the efflux activity of Daunorubicin (HY-13062A) and Rhodamine 123 (HY-D0816). P-gp modulator-6 can be used in the research of multidrug-resistant cancers. P-gp modulator-6 can be used in the research of multidrug-resistant pancreatic cancer and multidrug-resistant colon cancer.

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CAS. Nr.: 352652-36-9
Formel: C₁₆H₁₃ClN₂O₂
Molecular Weight:300.74

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

P-gp modulator-6 Chemical Structure

CAS. Nr.: 352652-36-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

P-gp

In Vitro

OthersAnti-cancer

Others

P-gp modulator-6 (compound 12) (10 μM; 2 h) more potently stimulates P-gp-mediated efflux of Daunorubicin (HY-13062A) than Rho-123 in mouse fibroblast Con A cells when used at 10 μM for 2 h^[1].

Anti-cancer

P-gp modulator-6 (5 days) exhibits similar antiproliferative activity against parental EPG85-257P and daunorubicin-resistant EPG85-257RDB gastric carcinoma cells, with reduced activity against Mitoxantrone (HY-13502)-resistant EPG85-257RNOV gastric carcinoma cells (IC₅₀ = 53.8 µM, RR = 2.51)^[2].
P-gp modulator-6 (5 days) exhibits antiproliferative activity against parental EPP85-181P pancreatic carcinoma cells, with reduced activity against daunorubicin-resistant EPP85-181RDB cells and increased activity against mitoxantrone-resistant EPP85-181RNOV cells (IC₅₀ = 33.6 µM, RR = 0.61)^[2].
P-gp modulator-6 (5 days) exhibits antiproliferative activity against parental HT-29P colon carcinoma cells, with a collateral sensitivity effect against daunorubicin-resistant HT-29RDB cells (IC₅₀ = 30.7 µM, RR = 0.50) and mitoxantrone-resistant HT-29RNOV cells (IC₅₀ = 19.3 µM, RR = 0.31)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

Human gastric carcinoma cell lines (parental EPG85-257P, daunorubicin-resistant EPG85-257RDB, mitoxantrone-resistant EPG85-257RNOV)
Concentration:

Dilution series
Incubation Time:

5 days
Result:

Exhibited antiproliferative activity against parental EPG85-257P cells with an IC₅₀ of 21.4 µM.
Showed similar antiproliferative activity against daunorubicin-resistant EPG85-257RDB cells with an IC₅₀ of 19.9 µM and a relative resistance ratio (RR) of 0.93.
Had reduced antiproliferative activity against mitoxantrone-resistant EPG85-257RNOV cells with an IC₅₀ of 53.8 µM and an RR of 2.51.

Cell Proliferation Assay^[2]

Cell Line:

Human pancreatic carcinoma cell lines (parental EPP85-181P, daunorubicin-resistant EPP85-181RDB, mitoxantrone-resistant EPP85-181RNOV)
Concentration:

Dilution series
Incubation Time:

5 days
Result:

Exhibited antiproliferative activity against parental EPP85-181P cells with an IC₅₀ of 55.1 µM.
Had reduced antiproliferative activity against daunorubicin-resistant EPP85-181RDB cells with an IC₅₀ of 85.6 µM and an RR of 1.55.
Showed increased antiproliferative activity against mitoxantrone-resistant EPP85-181RNOV cells with an IC₅₀ of 33.6 µM and an RR of 0.61.

Cell Proliferation Assay^[2]

Cell Line:

human colon carcinoma cell lines (parental HT-29P, daunorubicin-resistant HT-29RDB, mitoxantrone-resistant HT-29RNOV)
Concentration:

Dilution series
Incubation Time:

5 days
Result:

Exhibited antiproliferative activity against parental HT-29P cells with an IC₅₀ of 61.5 µM.
Showed increased antiproliferative activity against daunorubicin-resistant HT-29RDB cells with an IC₅₀ of 30.7 µM and an RR of 0.50.
Showed increased antiproliferative activity against mitoxantrone-resistant HT-29RNOV cells with an IC₅₀ of 19.3 µM and an RR of 0.31.

Chemical Information

CAS. Nr. 352652-36-9
Appearance Solid
Molecular Weight 300.74
Formel C₁₆H₁₃ClN₂O₂
Color Light brown to brown
SMILES

ClC1=CC=C(CC2=NOC(C3=C(OC)C=CC=C3)=N2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kondratov RV, et al. Small molecules that dramatically alter multidrug resistance phenotype by modulating the substrate specificity of P-glycoprotein. Proceedings of the National Academy of Sciences of the United States of America. 2001 Nov 20;98(24):14078-83. [Content Brief]

[2]. Ramalhete C, et al. Triterpenoids from Momordica balsamina with a Collateral Sensitivity Effect for Tackling Multidrug Resistance in Cancer Cells. Planta medica. 2018 Dec;84(18):1372-1379. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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P-gp modulator-6

Biologische Aktivität

Beschreibung

IC50 & Target

In Vitro

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

P-gp modulator-6 Related Classifications

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