Glycine, L-γ-glutaMyl-S-(diMethylarsino)-L-cysteinyl- Property

storage temp. 

Store at -20°C

solubility 

DMSO:10.0(Max Conc. mg/mL);24.31(Max Conc. mM)

form 

A crystalline solid

pka

2.21±0.10(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Glycine, L-γ-glutaMyl-S-(diMethylarsino)-L-cysteinyl- Chemical Properties,Usage,Production

Description

Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC₅₀s = 5-10 μM) and patient-derived primary prostate cancer cells (IC₅₀s = 2.5-20 μM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC₅₀s = 2.7 and 1.3 μM, respectively). It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G₂/M phase. Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 μM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation. Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.

Uses

Darinaparsin-d5 is the isotope labelled analog of Darinaparsin. Darinaparsin is an arsenic cytotoxin that has been used in pharmacological activities to evaluate the effect on survival an radiosensitivity of tumor cells in vitro under normoxia and hypoxia and in vivo using xenograft models. Darinaparsin has significant and preferential cytotoxic and radiosensitizing effects on solid tumors as compared with normal cells.?? Darinaparsin may therefore increase the therapeutic index of radiation therapy and has near term translational potential.

Definition

ChEBI: (2S)-2-amino-5-[[(2R)-1-(carboxymethylamino)-3-(dimethylarsinothio)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid is a peptide.