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Cat. No.: HY-119724

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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.

For research use only. We do not sell to patients.

CAS No.: 1942919-63-2
Formula: C₂₅H₂₀Cl₂N₂O₂
Molecular Weight:451.34

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

ABCG2-IN-3 Chemical Structure

CAS No.: 1942919-63-2

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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
MDCK-II	GI₅₀	4.67 μM Compound: 51	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	[PMID: 27280693]
MDCK-II	GI₅₀	4.83 μM Compound: 51	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	[PMID: 27280693]
Sf9	IC₅₀	0.026 μM Compound: 51	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	[PMID: 27280693]
Sf9	IC₅₀	0.285 μM Compound: 51	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	[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.

Chemical Information

CAS No. 1942919-63-2
Molecular Weight 451.34
Formula C₂₅H₂₀Cl₂N₂O₂
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

References

[1]. Spindler A, et al., Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). J Med Chem. 2016 Jul 14;59(13):6121-35. [Content Brief]

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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.

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ABCG2-IN-3

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ABCG2-IN-3 Related Classifications

HY-119724 Related Classifications