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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- 화학식: C28H33BF6N2O7
- 분자량:634.37
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 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. Further protocols information, click here.
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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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분자량 634.37
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anticancer agent 114 Related Classifications
HY-149832 Related Classifications
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