2. Metabolic Enzyme/Protease
  3. Proteasome
  4. 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.

For research use only. We do not sell to patients.

Anticancer agent 114 Chemical Structure

Anticancer agent 114 Chemical Structure

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Anticancer agent 114 Related Antibodies

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Description

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[1].

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.

Anticancer agent 114 Related Antibodies

Cell Viability Assay[1]

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 (compound 18u; 6 and 10 mg/kg; p.o.; twice a week, for 21 days) exhibits anticancer efficacy in human MM (RPMI-8226) xenograft mouse model[1].
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
Molecular Weight

634.37

Formula

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Anticancer agent 114 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Anticancer agent 114Anticancer agent114Anticancer agent-114Proteasomedipeptide boronic acid esterantiproliferativeRPMI-8226 cellsmultiple myelomaInhibitorinhibitorinhibit

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