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Bortezomib

Cat. No. M1686
Bortezomib Structure
Synonym:

Velcade; DPBA; LDP 341; MG 341; NSC 681239

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 40  USD40 In stock
10mg USD 58  USD58 In stock
50mg USD 110  USD110 In stock
100mg USD 160  USD160 In stock
200mg USD 256  USD256 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source INTERNATIONAL JOURNAL OF ONCOLOGY (2016) . Figure 9. Bortezomib (M1686) was from Abmole Bioscience Inc. (Houston, TX, USA)
Method FACS
Cell Lines B cells from CD19 cre/+Foxo1F/+ and CD19 cre/+Foxo1F/F mice
Concentrations 0.05 μg/ml
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)
Method FACS
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).
Protocol
Cell Experiment
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 384.24
Formula C19H25BN4O4
CAS Number 179324-69-7
Purity 99.27%
Solubility DMSO 72 mg/mL
Storage at -20°C
References

[1] Andrew Sandstrom, et al. Science. Functional degradation: A mechanism of NLRP1 inflammasome activation by diverse pathogen enzymes

[2] Ashley J Chui, et al. Science. N-terminal degradation activates the NLRP1B inflammasome

[3] Koda et al. Rinsho Ketsueki. Early onset of paralytic ileus caused by simultaneous administration of bortezomib and azole antifungals in multiple myeloma patients.

[4] Rushworth et al. Cell Signal. BTK inhibitor ibrutinib is cytotoxic to myeloma and potently enhances bortezomib and lenalidomide activities through NF-κB.

[5] Chauhan et al. Cancer Cell. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.

[6] Jung et al. Am J Hematol. Synergistic anticancer effects of arsenic trioxide with bortezomib in mantle cell lymphoma.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Bortezomib, Velcade; DPBA; LDP 341; MG 341; NSC 681239 supplier, Proteasome, inhibitors

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