Bortezomib Inhibitor CAS No. 179324-69-7

Cat. No.	Name	Size	Price
KI0328	Bortezomib	5 mg	$112
	Bortezomib	25 mg	$490
	Bortezomib	100 mg	$1280

Chemical Characteristic

Product Name	Bortezomib
Synonyms	Velcade, PS-341
CAS No.	179324-69-7
Molecular Weight	384.24
Formula	C₁₉H₂₅BN₄O₄
Chemical Name	[(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]-boronic acid
Smiles	[C@@H](CC(C)C)(NC(=O)[C@H](Cc1ccccc1)NC(=O)c1cnccn1)B(O)O
Chemical Structure

Biological activities

Bortezomib is a potent and selective inhibitor of the proteasome. The Ki of bortezomib against the chymotryptic activity of the 20S proteasome is 0.6 nM. ^[1] The IC50 values of bortezomib in MM.1S and MM.1R cells are 1.5 and 3 nM, respectively. Cell growth of Dox40, MR20, and LR5 MM cells is completely inhibited by bortezomib. The IC50 values of bortezomib in RPMI8226, Dox40, MR20, and LR5 are 0.03, 0.04, 0.02, and 0.02 μM, respectively. Bortezomib directly inhibits proliferation and induces apoptosis of human MM cell lines and freshly isolated MM cells. Bortezomib inhibits mitogen-activated protein kinase (MAPK) growth signaling in MM cells. Bortezomib induces apoptosis despite induction of p21 and p27 in both p53 wild-type and p53 mutant MM cells. Bortezomib also inhibits the paracrine growth of human MM cells by decreasing their adherence to bone marrow stromal cells (BMSCs) and related nuclear factor (NF) κB-dependent induction of interleukin-6 secretion in BMSCs, as well as inhibiting proliferation and growth signaling of residual adherent MM cells. Bortezomib inhibits TNFα-stimulated activation of NF-κB in primary HUVECs by blocking the degradation of the inhibitor IκBα. Bortezomib inhibits NF-κB activation in MM cells by stabilizing IκBα. Bortezomib also blocks the activation of MAPK, but not of STAT3, in MM cells adherent to BMSCs for 4 hours. ^[2] Bortezomib blocks not only nuclear translocation of NF-κB, but also NF-κB DNA binding, and demonstrates consistent antitumor activity against chemoresistant and chemosensitive myeloma cells. ^[3] Bortezomib can facilitate apoptosis by reducing expression and/or activity of survival factors, such as NF-κB, which results in decreased levels of Bcl-2 and Bcl-X_{L. Bcl-2 is overexpressed in up to 90% of small cell lung cancer (SCLC) tumors. ^[4] Bortezomib induces a significant inhibition of tumor growth, including several complete tumor regressions, and doubles the survival of treated mice compared with controls. In addition to inhibition of tumor growth and induction of apoptosis in vivo, bortezomib also decreases neovascularization of the tumor. ^[5] There is a 4??% loss of body weight in mice of both the bortezomib alone group and the combination group, whereas <2% change of body weight is seen in mice of both the PBS control group. After a 1-week recovery period, mice in the bortezomib-treated groups regain body weight, and the dosing regimen is then resumed for another 2 weeks.^[1]}

References

[1] Tan C, et al. Proteasome inhibitor PS-341, a potential therapeutic agent for adult T-cell leukemia. Cancer Res. 2002, 62(4): 1083-1086. [2] Hideshima T, et al. The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells. Cancer Res. 2001, 61(7): 3071-3076. [3] Ma MH,et al. The proteasome inhibitor PS-341 markedly enhances sensitivity of multiple myeloma tumor cells to chemotherapeutic agents. Clin Cancer Res. 2003, 9(3): 1136-1144. [4] Davies AM, et al. Incorporating bortezomib into the treatment of lung cancer. Clin Cancer Res. 2007, 13(15 Pt 2): s4647-s4651. [5] Cavo M. Proteasome inhibitor bortezomib for the treatment of multiple myeloma. Leukemia. 2006, 20(8): 1341-1352.

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