Anticancer agent 114
Anticancer agent 114 is a potent and orally active dipeptide boronic acid ester proteasome inhibitor with an IC50 value of 2.2 nM. Anticancer agent 114 has antiproliferative activity against the RPMI-8226 cells. Anticancer agent 114 can be used in research of multiple myeloma.
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- Fòrmula: C28H33BF6N2O7
- Peso molecular:634.37
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RPMI-8226 | IC50 |
5.6 nM
Compound: 18u
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Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer-Glo luminescence assay
Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer-Glo luminescence assay
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[PMID: 36806958] |
In Vitro
Anticancer agent 114 (compound 18u; 0-2 μM; 24 h) has antiproliferative activity against the RPMI-8226 cells with an IC50 value of 5.6 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RPMI-8226 cells
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Concentration:0-2 μM
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Incubation Time:24 hours
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Result:Inhibited cell growth in a dose-dependent manner.
In Vivo
Anticancer agent 114 (0.4 mg/kg and 1.2 mg/kg; i.v and p.o.; male Sprague-Dawley rats) exhibits good microsome stabilities and pharmacokinetic properties[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c nude mice with human MM (RPMI-8226) xenografts[1]
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Dosage:6 and 10 mg/kg
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Administration:oral administration; twice a week, for 21 days
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Result:Inhibited tumor growth in a dose-dependent manner.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:0.4 mg/kg and 1.2 mg/kg
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Administration:0.4 mg/kg (i.v.) and 1.2 mg/kg (p.o.)
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Result:
1.19 Dose i.v. (0.4 mg/kg) i.g. (1.2 mg/kg) Cmax (ng/mL) - 174 Tmax (h) - 0.83 T1/2 (h) 24.14 30 Cls 0.44 - AUC0-t (ng·h/mL) 2270 2680 F % - 34
Chemical Information
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Peso molecular 634.37
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Fòrmula C28H33BF6N2O7
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SMILES
CC(C[C@@H](B1OC2C3OC(C2(O1)C)CC3C(O)=O)NC(C(NC(C4=C(C=CC(C(F)(F)F)=C4)C(F)(F)F)=O)CC5CC5)=O)C
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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)
Anticancer agent 114 Related Classifications
HY-149832 Related Classifications
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