NSC636795
NSC636795 is an inhibitor of the ABCG2 transporter. NSC636795 inhibits ABCG2-mediated PhA efflux. NSC636795 also partially reverses ABCG2-mediated resistance to Topotecan (HY-13768). NSC636795 can be used in studies related to ABCG2-mediated antitumor drug resistance.
For research use only. We do not sell to patients.
- CAS No.: 66528-28-7
- Formula: C8H9N3OS2
- Molecular Weight:227.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
ABCG2 |
In Vitro
NSC636795 (20 μM; 10 min pre-incubation before IAAP addition) weakly inhibits the binding of [125I]IAAP to ABCG2 in crude membranes of MCF-7 FLV1000 cells, with an observed inhibition rate of 15%[1].
NSC636795 (10 μM; 30 min PhA incubation followed by 1 h efflux incubation) inhibits ABCG2-mediated PhA efflux in HEK 293 cells transfected with wild-type ABCG2, as evidenced by a 2.4-fold increase in intracellular PhA fluorescence intensity[1].
NSC636795 (10 μM; 96 h) partially reverses ABCG2-mediated topotecan resistance in HEK 293 cells transfected with wild-type ABCG2, reducing the relative resistance value from 19 to 4.9[1].
The combination of NSC636795 (10 μM; 96 h) with Topotecan partially reverses ABCG2-mediated Topotecan resistance in ABCG2-transfected HEK293 cells, reducing the relative resistance fold from 19 to 4.9; this concentration of NSC636795 results in less than 10% cell death in both empty vector-transfected and ABCG2-transfected cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type ABCG2-transfected HEK 293 cells, empty vector-transfected HEK 293 cells
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Concentration:10 μM
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Incubation Time:96 h
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Result:Reduced the relative resistance value of ABCG2-transfected cells to topotecan from 19 to 4.9.
Caused less than 10% cell death in both cell lines at 10 μM.
Chemical Information
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CAS No. 66528-28-7
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Molecular Weight 227.31
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Formula C8H9N3OS2
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SMILES
S=C(NNC(C1=CC=NC=C1)=O)SC
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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)