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Bortezomib

Description Drug for Cancer treatment
Bortezomib
Bortezomib structure
CAS No.
179324-69-7
Chemical Name:
Bortezomib
Synonyms
dpba;MLM341;VELCADE;Radiciol;BortezMib;BORTEZOMIB;BortezoMib R;BortezoMib-D8;MG-341 PS-341;BortezoMib Base
CBNumber:
CB8721789
Molecular Formula:
C19H25BN4O4
Formula Weight:
384.24
MOL File:
179324-69-7.mol

Bortezomib Properties

Melting point:
122-124°C
Density 
1.214
RTECS 
ED7771666
storage temp. 
Hygroscopic, -20°C Freezer, Under Inert Atmosphere
solubility 
Soluble in chloroform, dimethyl sulfoxide, ethanol and methanol.
pka
9.66±0.43(Predicted)
Stability:
Hygroscopic and Moisture Sensitive
CAS DataBase Reference
179324-69-7(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS06,GHS08
Hazard statements  H300-H310-H330-H372
Precautionary statements  P301+P310a-P304+P340-P320-P330-P405-P501a
Risk Statements  23/24/25-48/23/24/25
Safety Statements  9-27-36/37-45-60
HazardClass  6.1
HS Code  29339900

Bortezomib price More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Alfa Aesar J60378 Bortezomib, 99% 179324-69-7 10mg $200 2018-11-13 Buy
Alfa Aesar J60378 Bortezomib, 99% 179324-69-7 25mg $351 2018-11-13 Buy
Cayman Chemical 10008822 Bortezomib ≥95% 179324-69-7 1mg $25 2018-11-19 Buy
Cayman Chemical 10008822 Bortezomib ≥95% 179324-69-7 5mg $56 2018-11-19 Buy
Cayman Chemical 10008822 Bortezomib ≥95% 179324-69-7 10mg $100 2018-11-19 Buy

Bortezomib Chemical Properties,Uses,Production

Description

Bortezomib, a modified dipeptidyl boronic acid, is a therapeutic proteasome inhibitors used for the treatment of cancers. It is indicated for the treatment of relapsed multiple myeloma and mantle cell lymphoma. It is capable of inhibiting the mammalian 26S proteasome, which is important in regulating the intracellular concentration of specific proteins to maintain homeostasis within cells. The disruption of 26S proteasome function disrupts normal cellular homeostasis, leading to cytotoxic effect on various kinds of cancer cells. 

Drug for Cancer treatment

Bortezomib is a drug for treatment of hematopoietic malignancies with the appearance being white or white-like crystalline powder. It is easily soluble in dimethyl sulfoxide, ethanol, but insoluble in aqueous solution. This product is the reversible inhibitor of the mammal cell 26S proteasome chymotrypsin-like activity. 26S proteasome is a large protein complex which can degrade ubiquitin. Ubiquitin proteasome pathway plays an important role in regulation of the intracellular concentration of specific proteins in order to maintain the stability of the intracellular environment. Proteolytic affects intracellular multi-level signalling cascade. The disruption of the normal intracellular environment can lead to cell death while the inhibition of the 26S proteasome can prevent the hydrolysis of specific proteins. In vitro tests have proved bortezomib exhibits cytotoxicity to multiple types of cancer cells. The in vivo models of preclinical tumor have proved that bortezomib is capable of delaying the tumor growth of multiple myeloma which is suitable for the treatment of multiple myeloma.
The above information is edited by the Chemicalbook of Dai Xiongfeng.

Description

Bortezomib, a potent ubiquitin proteasome (26S) inhibitor (Ki=0.6 nM), was launched in the US as a treatment for multiple myeloma. This proteasome is required for the proteolytic degradation of the majority of cellular proteins and is present in all cells. It is required for the control of inflammatory processes, cell cycle regulation and gene expression and is a novel target in cancer treatment. Bortezomib is a N-acyl-pseudodipeptidyl boronic acid and formulated as a mannitol ester. Aldehyde containing peptides are also proteasome inhibitors, but lack chiral stability (racemization) and selectivity against other proteases including cysteine proteases. Replacement of the aldehyde moiety by a boronic acid avoids these shortcomings and provides some measure of selective proteasome inhibition relative to many other serine proteases. It is prepared by coupling the pinanediol ester of leucine boronic acid with N-tert-Bocphenylalanine utilizing O-(1H-benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate (TBTU) as the coupling agent. The tert-Boc protecting group is then cleaved from the dipeptide and pyrazinecarboxylic acid is coupled to form the terminal amide. Hydrolysis of the boronate ester is accomplished via a two-phase transesterification procedure using isobutyl boronic acid and aqueous extraction. In a study of patients who had received at least two prior therapies and demonstrated disease progression on their most recent therapy, about twenty eight percent showed a response to bortezomib. The response lasted a median time of one year. Another trial in 54 patients with relapsed multiple myeloma showed similar responses. It is dosed intravenously at an exposure of 1.3 mg/m2/dose twice weekly for two weeks followed by a 10-day drug-holiday. At therapeutic doses, the plasma drug levels were reported to drop to near detection limits within minutes of intravenous dosing. Based upon an ex vivo proteasome activity assay using blood cells, the pharmacodynamic half-life ranged from 9 to 15 h in patients with advanced malignancies.

Chemical Properties

Yellow Solid

Originator

Millenium (LeukoSite, Proscript) (US)

Uses

Bortezomib is the first proteasome inhibitor to be approved b the US FDA for multiple myeloma, a blood cancer. A reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. T

Definition

ChEBI: L-Phenylalaninamide substituted at the amide nitrogen by a 1-(dihydroxyboranyl)-3-methylbutyl group and at Nalpha by a pyrazin-2-ylcarbonyl group. It is a dipeptidyl boronic acid tha reversibly inhibits the 26S proteasome.

brand name

Velcade (Millennium).

General Description

Proteasomes normally function to degrade proteins that areno longer needed by the cell. Such proteins are normallymarked by the addition of ubiquitin, a 76 amino acid proteinthat is added to the -amino group of lysine residues onthe target proteins. The marked proteins are then hydrolyzedby the large barrel-shaped proteasomes to givepeptides of 7 to 8 residues that may be further hydrolyzedand reutilized by the cell. This process serves to regulateprotein levels within the cell, remove defective proteins,and becomes important in maintaining normal signal transduction.Inhibition of the proteasomes results in the buildup of ubiquitylated proteins, which disrupts cell-signalingprocesses and cell growth. The signaling bytranscription factor NF-B (nuclear factor B) appears tobe especially sensitive to bortezomib. NF-B is associatedwith the transcription of antiapoptotic and proliferativegenes but is under the control of IB (inhibitor of NF-B).IB can itself be phosphorylated by IKK (IB kinase),which marks IB for ubiquitylation and destruction allowingNF-B to mediate its antiapoptotic and proliferative effects effects.In the presence of the competitive inhibitor bortezomib(IC50=0.6 nM), the 26S proteasome is inhibitedand the ubiquitylated IkB is still capable of inhibiting NF-kB, preventing its effects.

Pharmaceutical Applications

Bortezomib belong to the class of drugs called proteasome inhibitors and is licensed in the United States and the United Kingdom for the treatment of multiple myeloma. The drug has been licensed for patients in whom the myeloma has progressed despite prior treatment or where a bone marrow transplant is not possible or was not successful. It is marketed under the name Velcade? or Cytomib?. Velcade is administered via injection and is sold as powder for reconstitution.
Bortezomib was the first drug approved in the new drug class of proteasome inhibitors and boron seems to be its active element. For the mode of action, it is believed that the boron atom binds with high affinity and specificity to the catalytic site of 26S proteasome and inhibits its action. Therapy with Bortezomib can lead to a variety of adverse reactions, including peripheral neuropathy, myelosuppression, renal impairment and gastrointestinal (GI) disturbances together with changes in taste. Nevertheless, the side effects are in most cases less severe than with alternative treatment options such as bone marrow transplantation.

Bortezomib Preparation Products And Raw materials

Raw materials

Preparation Products


Bortezomib Suppliers

Global( 387)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales01@yibaibiotech.com CHINA 411 58
Alpha Biopharmaceuticals Co., Ltd
0086-411-39042497
0086-411-39042693 sales@alphabiopharm.com China 921 58
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19918 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21671 58
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
alice@hbjkai.com CHINA 272 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sale@mainchem.com CHINA 32447 55

View Lastest Price from Bortezomib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-08-30 Bortezomib
179324-69-7
US $0.00 / Kg/Bag 10g 99% 800 kg hdzhl biotechnology co., ltd
2019-08-15 Bortezomib
179324-69-7
US $0.00-0.00 / KG 1g 99% 10kg/month Beijing Yibai Biotechnology Co., Ltd
2019-07-03 Bortezomib
179324-69-7
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.

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