A dimethylated arsenic linked to glutathione with anticancer activities; cytotoxic to DU145

Darinaparsin – 1 mg

Brand:
Cayman
CAS:
69819-86-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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).{39852,39851} It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase.{39852} 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.{39851} 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.{39852}  

 

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Description

A dimethylated arsenic linked to glutathione with anticancer activities; cytotoxic to DU145, LNCap, 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); decreases transcription of Gli-2 at 1.5 but not 3 µM; reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models at 100 mg/kg every other day

Formal name: L-γ-glutamyl-S-(dimethylarsino)-L-cysteinyl-glycine

Synonyms:  Dimethylarsinic glutathione|ZIO 101

Molecular weight: 411.3

CAS: 69819-86-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling

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