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Cat. No.: HY-400081

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F0161-0219

F0161-0219 is an ABCG2 inhibitor with a K_d value of 45.4 μM. F0161-0219 binds within the substrate transport channel, blocks efflux function, stabilizes the transporter, and retains Doxorubicin in the central cavity. F0161-0219 restores cellular sensitivity to Doxorubicin and increases the intracellular accumulation of multiple ABCG2 substrates. F0161-0219 can be used for research on breast cancer.

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

CAS No.: 329906-08-3
Formula: C₃₁H₂₁N₃O₂S
Molecular Weight:499.58

Storage:

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

F0161-0219 Chemical Structure

CAS No.: 329906-08-3

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC50	90.3 μM	Cytotoxicity against human MCF-7 breast cancer cells assessed as viability reduction incubated 48 hrs by absorbance measurement at 450 nm. Cytotoxicity against human MCF-7 breast cancer cells assessed as viability reduction incubated 48 hrs by absorbance measurement at 450 nm.	42734561

In Vitro

Anti-cancerOthers

Anti-cancer

F0161-0219 (48 h) exhibits low intrinsic cytotoxicity in MCF-7 and MCF-7/ADR cells, with IC₅₀ values of 90.3 and 79.9 μM^[1].

Others

F0161-0219 directly binds to ABCG2 with a K_d of 45.4 μM and protects ABCG2 from Pronase-mediated degradation in MCF-7/ADR lysates^[1].
F0161-0219 (20 μM; 2 h) inhibits ABCG2-mediated efflux of Doxorubicin (HY-15142A) in MCF-7/ADR and MDCKII-OVABCG2 cells, increasing intracellular Doxorubicin retention by 1.94-fold and 1.91-fold, respectively^[1].
F0161-0219 (5-20 μM; 48 h) concentration-dependently restores the accumulation of Mitoxantrone (HY-13502) and Hoechst 33342 (HY-15559) in MCF-7/ADR and MDCKII-OVABCG2 cells^[1].

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

Related Protocols :

Breast Cancer Modeling

Chemical Information

CAS No. 329906-08-3
Molecular Weight 499.58
Formula C₃₁H₂₁N₃O₂S
SMILES

O=C(C1=CC=C2C=CC=CC2=C1)NC3=NC(C4=CC=CC(NC(C5=CC=C6C=CC=CC6=C5)=O)=C4)=CS3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Li H, et al. Leveraging a Deep Learning Model and Computational Screening for the Discovery of ABCG2 Inhibitors against Drug-Resistant Breast Cancer. Journal of chemical information and modeling. 2026 Sep 14;66(17):11174-11190.

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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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