ABCG2-IN-3
ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC50 of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the ATPase activity.
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- CAS No.: 1942919-63-2
- Formule: C25H20Cl2N2O2
- Masse moléculaire:451.34
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDCK-II | GI50 |
4.67 μM
Compound: 51
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Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 27280693] |
| MDCK-II | GI50 |
4.83 μM
Compound: 51
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Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 27280693] |
| Sf9 | IC50 |
0.026 μM
Compound: 51
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Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method
Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method
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[PMID: 27280693] |
| Sf9 | IC50 |
0.285 μM
Compound: 51
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Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method
Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method
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[PMID: 27280693] |
In Vitro
ABCG2-IN-3 exhibits a cytotoxicity against cells MDCK II BCRP and MDCK wild-type, with CI50s of 5.82 and 6.55 μM[1].
ABCG2-IN-3 inhibits ATPase with an IC50 of 0.038 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1942919-63-2
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Masse moléculaire 451.34
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Formule C25H20Cl2N2O2
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SMILES
COC1=CC=C(C=C1)C(N2C(C3=C(CC2)C(C=CC=C4)=C4N3)C5=CC(Cl)=C(C=C5)Cl)=O
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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.
Protocole
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ABCG2-IN-3 Related Classifications
HY-119724 Related Classifications
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