ALVOCIDIB HCl

(−)-2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1- benzopyran- 4-one hydrochloride; Alvocidib; Flavopiridol hydrochloride; cis-(-)-2-(2-Chlorophenyl)- 5,7-dihydroxy- 8-(3-hydroxy- 1-methyl-4-piperidinyl)-4H-1-benzopyran-4-one;

 ALVOCIDIB HCl

 

PRODUCT IDENTIFICATION

CAS RN

146426-40-6, 131740-09-5 (HCl)

EINECS RN

 

FORMULA

C21H20ClNO5·HCl

MOLE WEIGHT

438.30

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE

yellow powder

MELTING POINT

 

BOILING POINT

 

DENSITY

 

SOLUBILITY IN WATER

2mg/ml (Soluble in DMSO)

pH

 

VAPOR DENSITY

 

REFRACTIVE INDEX

 

FLASH POINT

 

 

STABILITY AND REACTIVITY
STABILITY Stable under normal conditions

INCOMPATIBLE MATERIALS

Strong oxidizing agents

DECOMPOSITION PRODUCTS

Carbon oxides. Nitrogen oxides. Hydrogen chloride gas

POLYMERIZATION Has not been reported

NFPA RATINGS

Health: 1, Flammability: 0, Reactivity: 0

 

SAFETY

HAZARD NOTES

Harmful. Do not breathe dust.

EYE

May cause eye irritation.

SKIN

May be harmful if absorbed through skin. May cause skin irritation.

INGESTION

May be harmful if swallowed.

INHALATION

May be harmful if inhaled. May cause respiratory tract irritation.

CHRONIC

 

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

 
HAZARD CLASS

 

PACKING GROUP

 

HAZARD CODE

XN

RISK STATEMENTS

22

SAFETY STATEMENTS

 

 

EXTERNAL LINKS & GENERAL INFORMATION
Alvocidib; A synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) (http://www.cancer.gov/)

Flavopiridol is effective in inducing cell cycle arrest and cytotoxicity in rhabdoid tumors. Its effects are correlated with the down-regulation of cyclin D1 and the up-regulation of p21. Flavopiridol is potentially a novel chemotherapeutic agent for rhabdoid tumors. (http://clincancerres.aacrjournals.org/)

In general, pharmacological inhibitors of CDKs display selective anti-proliferative effects on cycling cells, especially tumor cells. Depending on the selectivity profile, growth arrest in G0/G1 (CDK4/6-selective) or in G1/S and G2/M (pan-CDK- and CDK1/2-selective) is observed. More importantly, many compounds, especially potent CDK2 inhibitors, have been observed to induce apoptosis selectively in transformed cells [62]. As discussed above, many compounds with very high potency against CDKs in vitro are available. However, in many cases this biochemical potency does not translate into cellular potency, presumably due to unknown mechanistic reasons and perhaps because of high physiological ATP concentrations. Connected with this problem is the question of what are the actual cellular targets of a biochemical CDK inhibitor. One technique that has been applied to CDK inhibitors is affinity chromatography of cell lysates on immobilized inhibitor preparations. Indeed it was found that, apart from CDKs, other proteins were also bound. (http://www.sigmaaldrich.com/)

 

SALES SPECIFICATION

APPEARANCE

yellow powder

ASSAY

98.0% min

 

PRICE INFORMATION