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Bortezomib



Chemical Properties of 'Bortezomib'

CAT No. :

CS-O-00482
CAS Registry No. : 179324-69-7
Category : API Standards
Molecular Weight: 384.24
Molecular Formula : C₁₉H₂₅BN₄O₄



OTHER INFORMATION of 'Bortezomib'
Purity : Not less than 95 %
Therapeutic : Synthetic Peptides
Purity : Not less than 95 %
Therapeutic : Synthetic Peptides
IUPAC Name :[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
Applicationnotes :"Bortezomib is the first proteasome inhibitor to be approved by 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."
Synonym :Not available
References :"Nawrocki; S,T,; et al: Cancer Research; 65; 11510 (2005); Drahl C,: Chem, and Eng, News; 87; 41 (2009)"
Smileys :O=C(N[C@H](B(O)O)CC(C)C)[C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2
Appearance :White to off white solid
Color / Form :Powder
Melting Point :139-143
Solubility :The solubility of bortezomib, as the monomeric boronic acid, is 3.3 to 3.8 mg/mL in a pH range of 2 to 6.5.
Use Classification :Human drugs -> Velcade -> EMA Drug Category
Hazard Class :Acute Tox. 2 (97.09%)
UNII :69G8BD63PP
NCI Thesaurus Code :C1851
RXCUI :358258
MeSH Entry Terms :341, PS
Other Synonyms :Bortezomib
Removed Synonyms :Zindoxifene
Vapor Pressure : 5.1X10-20 mm Hg at 25 °C (est)
Other Experimental Properties :Hydroxyl radical reaction rate constant = 2.6X10-11 cu cm/molec-sec at 25 °C (est)
Label Ingredient : BORTEZOMIB
NDC Code :43598-865-60, 63020-049-01, 63323-721-10
Disposal Methods :SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.
Toxicity Summary :The Lowest published toxic dose (TDLo) in mouse was 5 mg/kg/14D following intraperitoneal administration of an intermittent dose and 1.6 mg/kg/12D following subcutaneous administration of a continuous dose. The therapeutic dose of bortezomib is individualized in each patient to prevent overdose. Fatal outcomes occurred in humans following the administration of more than twice the recommended therapeutic dose of bortezomib. The symptoms from overdose included the acute onset of symptomatic hypotension and thrombocytopenia. As there is no known antidote for bortezomib overdosage, monitoring of vital signs and appropriate supportive care should be initiated when drug overdosage is suspected. In monkeys and dogs, increased heart rate, decreased contractility, hypotension, and death were observed with the intravenous dose as low as two times the recommended clinical dose on a mg/m2 basis. A case of a slight increase in the corrected QT interval leading to death occurred in dog studies.
Hepatotoxicity :In large clinical trials of bortezomib, elevations in serum aminotransferase levels were common, occurring in ~10% of patients. However, values greater than 5 times the upper limit of normal (ULN) were rare, occurring in
Drug Induced Liver Injury :bortezomib
Interactions :Hypoglycemia and hyperglycemia have been reported in patients with diabetes mellitus who received bortezomib concomitantly with oral antidiabetic agents. If bortezomib is used concomitantly with oral antidiabetic agents, blood glucose concentrations should be monitored carefully and dosage of the antidiabetic agent adjusted as necessary.
Antidoteand Emergency Treatment :Maintain an open airway and assist ventilation if necessary. Treat coma, seizures, hypotension, and arrhythmias if they occur. Treat nausea and vomiting with metoclopramide and fluid loss caused by gastroenteritis with intravenous crystalloid fluids. Bone marrow depression should be treated with the assistance of an experienced hematologist or oncologist. Extravasation: Immediately stop the infusion and withdraw as much fluid as possible by negative pressure on the syringe. ... /For/ decontamination administer activated charcoal orally if conditions are appropriate. Gastric lavage is not necessary after small to moderate ingestions if activated charcoal can be given promptly. Because of the rapid intracellular incorporation of these agents, dialysis and other extracorporeal removal procedures are generally not effective.
Human Toxicity Excerpts :/SIGNS AND SYMPTOMS/ In humans, fatal outcomes following the administration of more than twice the recommended therapeutic dose have been reported, which were associated with the acute onset of symptomatic hypotension and thrombocytopenia. In the event of an overdosage, the patient's vital signs should be monitored and appropriate supportive care given.
Non Human Toxicity Excerpts :/LABORATORY ANIMALS: Acute Exposure/ Studies in monkeys showed that administration of dosages approximately twice the recommended clinical dose resulted in heart rate elevations, followed by profound progressive hypotension, bradycardia, and death 12 to 14 hours post dose. Doses =1.2 mg/sq m induced dose-proportional changes in cardiac parameters. Bortezomib has been shown to distribute to most tissues in the body, including the myocardium. Bortezomib doses as low as 2 times the recommended clinical dose on a mg/sq m basis were associated with increases in heart rate, decreases in contractility, hypotension, and death.
Protein Binding :Over the concentration range of 100 to 1000 ng/mL, bortezomib is about 83% bound to human plasma proteins.
Milk Concentrations :It is not known whether bortezomib is excreted in human milk.
Exact Mass :384.1968855
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
InchIKey :GXJABQQUPOEUTA-RDJZCZTQSA-N
Canonical SMILES :B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
Isomeric SMILES :B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
Product Description :Bortezomib is l-Phenylalaninamide substituted at the amide nitrogen by a 1-(dihydroxyboranyl)-3-methylbutyl group and at N(alpha) by a pyrazin-2-ylcarbonyl group. It is a dipeptidyl boronic acid that reversibly inhibits the 26S proteasome. It has a role as an antineoplastic agent, a proteasome inhibitor, a protease inhibitor and an antiprotozoal drug. It is an amino acid amide, a member of pyrazines and a L-phenylalanine derivative. It derives from a boronic acid.
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 15-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 15-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back


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What is Bortezomib ?
Bortezomib falls under API Standards of Bortezomib."Bortezomib is the first proteasome inhibitor to be approved by 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."
What is the CAS Number of Bortezomib?
The CAS Number of Bortezomib is 179324-69-7
Who are the suppliers of Bortezomib?
CLEARSYNTH is a worldwide supplier of Bortezomib

Related compounds of Bortezomib

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