CRT0093964
CRT0093964 is an isoform-selective non-carboxylate inhibitor of AKR1C3 (IC50=0.11 μM) with no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, and COX-2.CRT0093964 can be used for the research of leukemia, hormone-related cancers, colon cancer.
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- No. CAS: 700856-05-9
- Fòrmula: C15H20ClN3O2
- Peso molecular:309.79
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
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AKR1C3 0.11 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.018 μM
Compound: 24
|
Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs
Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs
|
[PMID: 24411201] |
In Vitro
CRT0093964 (0.1 nM-100 μM; 1 h) potently and selectively inhibits purified recombinant AKR1C3 with an IC50 of 0.11 μM; in contrast, this compound shows no inhibitory effect on AKR1C1, AKR1C2 or AKR1C4 at concentrations up to 30 μM[1].
CRT0093964 (1 nM-3 μM; 2 h pre-treatment) inhibits AKR1C3-dependent metabolism of PR-104A (HY-16405) in AKR1C3-overexpressing HCT-116 cells, with an IC50 of 0.018 μM, and exhibits higher potency in cellular assays than in purified enzyme assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 700856-05-9
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Peso molecular 309.79
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Fòrmula C15H20ClN3O2
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SMILES
O=C(N1CCOCC1)N2CCN(C3=CC=C(Cl)C=C3)CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)