OAT-4828
OAT-4828 is an orally active ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 32 nM. OAT-4828 induces antileukemic activity in B-cell-derived non-Hodgkin's lymphoma models via inhibition of USP7. OAT-4828 is applicable to research related to chronic lymphocytic leukemia.
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- No. CAS: 2947497-65-4
- Fòrmula: C28H28F3N5O3S
- Peso molecular:571.61
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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
[1]|
USP7 32 nM (IC50) |
In Vitro
OAT-4828 inhibits hERG potassium channels with an IC50 of 36 μM in a binding assay and 7.4 μM in a QPatch assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | AUC0-inf | T1/2 | Bioavailability | CL | Vss |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 3 mg/kg | i.v. | / | / | 1324 ng·h/mL | 0.45 h | / | 37.8 mL/min/kg | 0.9 L/kg |
| Mice[1] | 10 mg/kg | p.o. | 0.5 h | 172 ng/mL | 516 ng·h/mL | 0.92 h | 12 % | / | / |
| Rat[1] | 3 mg/kg | i.v. | / | / | 792 ng·h/mL | 5.0 h | / | 64.1 mL/min/kg | 12.7 L/kg |
| Rat[1] | 10 mg/kg | p.o. | 2 h | 53.6 ng/mL | 352 ng·h/mL | 5.0 h | 13 % | / | / |
| Rat[1] | 50 mg/kg | p.o. | 4 h | 1158 ng/mL | 5262 ng·h/mL | 2.9 h | / | / | / |
| Dog[1] | 3 mg/kg | i.v. | / | / | 979 ng·h/mL | 4.4 h | / | 51.7 mL/min/kg | 12.7 L/kg |
| Dog[1] | 10 mg/kg | p.o. | 2 h | 526 ng/mL | 3564 ng·h/mL | 4.5 h | 109 % | / | / |
| Dog[1] | 50 mg/kg | p.o. | 2 h | 3367 ng/mL | 26615 ng·h/mL | 6.0 h | / | / | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL6/J (female, 6−12 weeks old, adoptive transfer of 5×106 leukemic CD5+CD19+ TCL1 cells via tail vein injection)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily for 21 days
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Result:Reduced the percentage of leukemic CD5+CD19+ cells in blood by up to 74% on day 17 compared to vehicle control.
Significantly reduced spleen weight relative to vehicle control on day 21.
Caused no significant body weight loss.
Chemical Information
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No. CAS 2947497-65-4
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Peso molecular 571.61
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Fòrmula C28H28F3N5O3S
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SMILES
CN[C@H]1CCN(C1)C(C2=C(C=C(N=C2C3=C4SC(CN5C(C6C(C6(C)C)C5=O)=O)=CC4=NC=C3)C(F)(F)F)C)=O
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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)
OAT-4828 Related Classifications
HY-183689 Related Classifications
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