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???,L-γ-????-S-(???????)-L-?????-

???,L-γ-????-S-(???????)-L-?????-
???,L-γ-????-S-(???????)-L-?????- ??? ???
?? ??:
69819-86-9
???:
???,L-γ-????-S-(???????)-L-?????-
???(??):
???,L-γ-????-S-(???????)-L-?????-
???:
Glycine, L-γ-glutaMyl-S-(diMethylarsino)-L-cysteinyl-
???(??):
Darinaparsin;SP02);ZIO 101;EOS-60608;Selurampanel;Darinaparsin (ZIO101;Dimethylarsinic glutathione;Glycine, L-γ-glutaMyl-S-(diMethylarsino)-L-cysteinyl-
CBNumber:
CB42563431
???:
C12H22AsN3O6S
??? ??:
411.3
MOL ??:
69819-86-9.mol

???,L-γ-????-S-(???????)-L-?????- ??

?? ??
Store at -20°C
???
DMSO:10.0(Max Conc. mg/mL);24.31(Max Conc. mM)
??? ??
??? ??
?? ?? (pKa)
2.21±0.10(Predicted)
??
White to off-white
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H302 ??? ??? ?? ?? ?? - ?? ?? 4 ?? GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P280 ????/???/???/?????? ?????.
P301+P312 ??? ???? ??? ????(??)? ??? ????.
P302+P352 ??? ??? ??? ?? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
4 0

???,L-γ-????-S-(???????)-L-?????- C??? ??, ??, ??

??

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.

???,L-γ-????-S-(???????)-L-?????- ?? ?? ? ???

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???,L-γ-????-S-(???????)-L-?????- ?? ??

???( 28)?? ??
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