S34-1040
S34-1040 is an AKR1C3 inhibitor with a human IC50 of 0.03 μM and exhibits no detectable inhibition of AKR1C1, AKR1C2, or AKR1C4. S34-1040 functions as a chemosensitizer and restores sensitivity of doxorubicin-resistant breast cancer cells to doxorubicin. S34-1040 can be used for the research of doxorubicin-resistant breast cancer.
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- CAS No.: 3099381-90-2
- Formule: C18H17N3O2
- Masse moléculaire:307.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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AKR1C3 0.03 μM (IC50) |
S34-1040 potently and selectively inhibits recombinant AKR1C3 with an IC50 of 0.03 μM, and exhibits over 2500-fold selectivity over the structurally related AKR1C1, AKR1C2 and AKR1C4 isoforms[1].
S34-1040 (0-100 μM; 72-96 h) alone does not inhibit the proliferation of MCF-7/DOX cells even at a concentration as high as 100 μM. However, when treated with a protocol of 10-50 μM pre-incubation for 24 h followed by combined treatment for 72 h, it exerts strong synergistic effects with Doxorubicin (HY-15142A) to restore chemosensitivity, with a combination index (CI) ranging from 0.176 to 0.562[1].
Combined treatment with S34-1040 (10 μM; 14 days) and Doxorubicin completely inhibits long-term colony formation of MCF-7/DOX cells, whereas S34-1040 alone has no effect on clonogenic growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:doxorubicin-resistant MCF-7/DOX breast cancer cells
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Concentration:0, 5, 10, 25, 40, 60, 80, 100 μM (single-agent); 0, 10, 25, 50 μM μM (combination with 0, 10, 25, 50 μM Doxorubicin)
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Incubation Time:72-96 h (single-agent); 24 h pre-incubation, followed by 72 h co-treatment (combination)
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Result:Showed weak antiproliferative activity even at concentrations up to 100 μM, with good cellular safety as a single agent.
Produced significantly stronger antiproliferative effects than Doxorubicin alone across all tested concentrations when combined with Doxorubicin.
Demonstrated strong to very strong synergy between S34-1040 and doxorubicin, with combination index (CI) values ranging from 0.176 to 0.562.
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Cell Line:doxorubicin-resistant MCF-7/DOX breast cancer cells
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Concentration:10 μM (single-agent); 10 μM combined with 25 μM Doxorubicin
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Incubation Time:14 days
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Result:Significantly suppressed the colony-forming ability of MCF-7/DOX cells, with no visible colonies remaining when combined with Doxorubicin.
Showed no significant difference compared to the blank control when used alone.
Saw doxorubicin alone at 25 μM fail to completely inhibit colony formation.
Chemical Information
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CAS No. 3099381-90-2
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Masse moléculaire 307.35
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Formule C18H17N3O2
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SMILES
N#CC1=CC=C(C=C1)CN(C)C(C2=CC(C(C3CC3)=O)=CN2)=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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S34-1040 Related Classifications
HY-184928 Related Classifications
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