Bortezomib
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| Category | Antineoplastic |
| Catalog number | BBF-05860 |
| CAS | 179324-69-7 |
| Molecular Weight | 384.24 |
| Molecular Formula | C19H25BN4O4 |
| Purity | >98% |
Ordering Information
| Catalog Number | Size | Price | Stock | Quantity |
|---|---|---|---|---|
| BBF-05860 | 1 g | $398 | In stock |
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Add to cartDescription
Bortezomib is a potent, reversible and selective 20S proteasome inhibitor with a Ki of 0.6 nM. It is an antineoplastic agent that is used in treatment of refractory multiple myeloma and certain lymphomas.
Specification
| Synonyms | PS-341; PS 341; PS341; LDP 341; LDP-341; LDP341; MLN341; MLN-341; MLN 341; B-[(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid; Velcade; ((R)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid; N-[(1R)-1-(Dihydroxyboryl)-3-methylbutyl]-Nα-(2-pyrazinylcarbonyl)-L-phenylalaninamide |
| Storage | Store at -20°C |
| IUPAC Name | [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid |
| Canonical SMILES | B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O |
| InChI | InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1 |
| InChI Key | GXJABQQUPOEUTA-RDJZCZTQSA-N |
Properties
| Appearance | White crystalline powder |
| Antibiotic Activity Spectrum | Neoplastics (Tumor) |
| Boiling Point | N/A |
| Melting Point | >122°C |
| Density | 1.214±0.1 g/cm3 |
| Solubility | Soluble in Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly) |
Reference Reading
1.Bortezomib and etoposide combinations exert synergistic effects on the human prostate cancer cell line PC-3.
Aras B1, Yerlikaya A2. Oncol Lett. 2016 May;11(5):3179-3184. Epub 2016 Mar 16.
Novel treatment modalities are urgently required for androgen-independent prostate cancer. In order to develop an alternative treatment for prostate cancer, the cytotoxic effects of the 26S proteasome inhibitor bortezomib, either alone or in combination with the two commonly used chemotherapeutic agents irinotecan and etoposide, on the human prostate cancer cell line PC-3 were evaluated in the present study. The PC-3 cell line was maintained in Dulbecco's modified Eagle's medium with 10% fetal bovine serum and treated with various doses of bortezomib, irinotecan, etoposide or their combinations. The growth inhibitory and cytotoxic effects were determined by water-soluble tetrazolium (WST)-1 assay, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay or iCELLigence system. The combination index values were determined by the Chou-Talalay method. The half maximal inhibitory concentration (IC50) value of bortezomib on the PC-3 cell line was determined to be 53.
2.Liposomal bortezomib is active against chronic myeloid leukemia by disrupting the Sp1-BCR/ABL axis.
Yang X1,2,3, Pang J1, Shen N1, Yan F1, Wu LC2, Al-Kali A3, Litzow MR3, Peng Y4, Lee RJ5, Liu S1. Oncotarget. 2016 Apr 20. doi: 10.18632/oncotarget.8871. [Epub ahead of print]
The abundance of the BCR/ABL protein critically contributes to CML pathogenesis and drug resistance. However, understanding of molecular mechanisms underlying BCR/ABL gene regulation remains incomplete. While BCR/ABL kinase inhibitors have shown unprecedented efficacy in the clinic, most patients relapse. In this study, we demonstrated that the Sp1 oncogene functions as a positive regulator for BCR/ABL expression. Inactivation of Sp1 by genetic and pharmacological approaches abrogated BCR/ABL expression, leading to suppression of BCR/ABL kinase signaling and CML cell proliferation. Because of potential adverse side effects of bortezomib (BORT) in imatinib-refractory CML patients, we designed a transferrin (Tf)-targeted liposomal formulation (Tf-L-BORT) for BORT delivery. Cellular uptake assays showed that BORT was efficiently delivered into K562 cells, with the highest efficacy obtained in Tf-targeted group. After administered into mice, L-BORT exhibited slower clearance with less toxicity compared to free BORT.
3.Bortezomib and etoposide combinations exert synergistic effects on the human prostate cancer cell line PC-3.
Aras B1, Yerlikaya A2. Oncol Lett. 2016 May;11(5):3179-3184. Epub 2016 Mar 16.
Novel treatment modalities are urgently required for androgen-independent prostate cancer. In order to develop an alternative treatment for prostate cancer, the cytotoxic effects of the 26S proteasome inhibitor bortezomib, either alone or in combination with the two commonly used chemotherapeutic agents irinotecan and etoposide, on the human prostate cancer cell line PC-3 were evaluated in the present study. The PC-3 cell line was maintained in Dulbecco's modified Eagle's medium with 10% fetal bovine serum and treated with various doses of bortezomib, irinotecan, etoposide or their combinations. The growth inhibitory and cytotoxic effects were determined by water-soluble tetrazolium (WST)-1 assay, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay or iCELLigence system. The combination index values were determined by the Chou-Talalay method. The half maximal inhibitory concentration (IC50) value of bortezomib on the PC-3 cell line was determined to be 53.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
