Bortezomib (PS-341) is a highly selective, reversible inhibitor of the 26S proteasome with a ki value of 6nM, which has shown high antimyeloma activity. Bortezomib caused comparable growth suppression in LNCaP-Pro5 and PC3M-Pro4 cells with an IC90 of 10 nM.
Sci Rep. 2020 Feb 25;10(1):3386.
Gender-specific Changes in Energy Metabolism and Protein Degradation as Major Pathways Affected in Livers of Mice Treated With Ibuprofen
Bortezomib (PS-341) purchased from AbMole
Cell Physiol Biochem. 2018;50(6):2341-2364.
Peperomin E Induces Promoter Hypomethylation of Metastatic-Suppressor Genes and Attenuates Metastasis in Poorly Differentiated Gastric Cancer.
Bortezomib (PS-341) purchased from AbMole
Int J Oncol. 2016 Oct;49(4):1469-78.
Metabotropic glutamate receptor 3 is involved in B-cell-related tumor apoptosis
Bortezomib (PS-341) purchased from AbMole
Cell Experiment | |
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Cell lines | Nine canine melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML) |
Preparation method | Cell growth inhibition assay Nine canine melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML) were cultured in 96-well plates (2 *102 cells/well) for 24 h in cDMEM and treated with different concentrations of bortezomib (0–100 nM) for 72 h. Cell viability was then measured by a WST-1 cell proliferation assay kit (Takara) and the half maximal inhibitory concentration (IC50) of bortezomib for each cell line was calculated using the GraphPad Prism software (GraphPad Software). |
Concentrations | 0–100 nM |
Incubation time | 72 h |
Animal Experiment | |
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Animal models | CMM-1 cells in xenograft mouse models |
Formulation | 100 µL PBS containing 4.2% DMSO |
Dosages | 0.8mg/kg twice weekly |
Administration | intravenous(IV) injections |
Molecular Weight | 384.24 |
Formula | C19H25BN4O4 |
CAS Number | 179324-69-7 |
Solubility (25°C) | DMSO 72 mg/mL |
Storage | 2-8°C, protect from light |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Ashley J Chui, et al. Science. N-terminal degradation activates the NLRP1B inflammasome
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LXE408
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Zetomipzomib
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PI-1840
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Ixazomib Citrate (MLN9708)
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