Bortezomib (Velcade) 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.
|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).|
|Incubation time||72 h|
|Animal models||CMM-1 cells in xenograft mouse models|
|Formulation||100 µL PBS containing 4.2% DMSO|
|Dosages||0.8mg/kg twice weekly|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Source||INTERNATIONAL JOURNAL OF ONCOLOGY (2016) . Figure 9. Bortezomib (M1686) was from Abmole Bioscience Inc. (Houston, TX, USA)|
|Cell Lines||B cells from CD19 cre/+Foxo1F/+ and CD19 cre/+Foxo1F/F mice|
|Incubation Time||24 h|
|Results||The effect of Foxo1-defciency on cell apoptosis was approved by using B cells from CD19cre/+Foxo1F/+ and CD19cre/+Foxo1F/F (Fig. 9D).|
|Source||INTERNATIONAL JOURNAL OF ONCOLOGY (2016) . Figure 5. MBortezomib (M1686) was from Abmole Bioscience Inc. (Houston, TX, USA)|
|Cell Lines||SP2/0 cells|
|Concentrations||0, 0.05 and 0.25 μg/ml|
|Incubation Time||24 h|
|Results||Low dose of bortezomib, frst-line drug in patients with newly diagnosed multiple myeloma, could effectively induce apoptosis and Grm3 expression (Fig. 5).|
Int J Oncol. 2016 Oct;49(4):1469-78.
Metabotropic glutamate receptor 3 is involved in B-cell-related tumor apoptosis
Bortezomib purchased from AbMole
Early onset of paralytic ileus caused by simultaneous administration of bortezomib and azole antifungals in multiple myeloma patients.
Koda et al. Rinsho Ketsueki. 2012 Aug;53(8):760-4. PMID: 22975816.
BTK inhibitor ibrutinib is cytotoxic to myeloma and potently enhances bortezomib and lenalidomide activities through NF-κB.
Rushworth et al. Cell Signal. 2012 Sep 10. PMID: 22975686.
A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.
Chauhan et al. Cancer Cell. 2012 Sep 11;22(3):345-58. PMID: 22975377.
Synergistic anticancer effects of arsenic trioxide with bortezomib in mantle cell lymphoma.
Jung et al. Am J Hematol. 2012 Aug 2. PMID: 22965904.
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