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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C28H33BF6N2O7
- Masse moléculaire:634.37
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RPMI-8226 | IC50 |
5.6 nM
Compound: 18u
|
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
|
[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.
-
Cell Line:RPMI-8226 cells
-
Concentration:0-2 μM
-
Incubation Time:24 hours
-
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.
-
Animal Model:Female Balb/c nude mice with human MM (RPMI-8226) xenografts[1]
-
Dosage:6 and 10 mg/kg
-
Administration:oral administration; twice a week, for 21 days
-
Result:Inhibited tumor growth in a dose-dependent manner.
-
Animal Model:Male Sprague-Dawley rats[1]
-
Dosage:0.4 mg/kg and 1.2 mg/kg
-
Administration:0.4 mg/kg (i.v.) and 1.2 mg/kg (p.o.)
-
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
-
Masse moléculaire 634.37
-
Formule C28H33BF6N2O7
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
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)
Anticancer agent 114 Related Classifications
HY-149832 Related Classifications
Powered by Bioz