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.
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
|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).|
|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.
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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