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.
For research use only. We do not sell to patients.
- CAS No.: 2947497-65-4
- Formula: C28H28F3N5O3S
- Molecular Weight:571.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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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CAS No. 2947497-65-4
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Molecular Weight 571.61
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Formula 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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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OAT-4828 Related Classifications
HY-183689 Related Classifications
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