Molecular Formula | C18H24N2OS |
Molar Mass | 316.46 |
Solubility | DMSO: at 26 mg/mlsoluble |
Appearance | Orange-yellow solid |
Color | Yellow |
Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
Stability | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
MDL | MFCD00236450 |
Physical and Chemical Properties | Yellow powder, soluble in DMSO (up to 100 mM). |
Use | Tyrphostin AG 879 |
In vitro study | AG879 inhibited the growth of FET6αS26X cells in a concentration-dependent manner. AG879(10 nM) blocks the activation of PAK1 and inhibits RAS-induced carcinogenesis of NIH 3T3 cells. AG879(<1 μm) inhibited Tyr phosphorylation of ERK and Association of ERK with PAK1 in transformed NIH 3T3 fibroblasts by v-Ha-RAS. AG 879 dose-dependently reduced MCF-7 cell number and has shown a significant effect at 0.4 mM by inhibiting DNA synthesis and mitosis. AG 879(<20 μm) inhibited MCF-7/2 activation in ERK-1 cells. AG 879(5 μm) reduced the expression of Hsp90 client protein RAF-1 and HER-2. In human leiomyosarcoma (HTB-114,HTB-115,HTB-88), rhabdomyosarcoma (HTB-82,TE-671), prostate cancer (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937) in cell lines, AG879(20 μm) significantly reduced cell proliferation and increased apoptosis to varying degrees. |
In vivo study | AG879(2 mg) reduced tumor growth in HTB-114 or HL-60 athymic NOD/SCID mice transplanted. In nude mice harboring v-Ha-RAS transformed NIH 3T3 cells, AG 879(20 mg/kg) treatment completely protected 50% of mice from RAS-Induced Sarcoma and significantly reduced the size of the growing sarcoma. |
WGK Germany | 3 |
HS Code | 29309090 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.16 ml | 15.8 ml | 31.6 ml |
5 mM | 0.632 ml | 3.16 ml | 6.32 ml |
10 mM | 0.316 ml | 1.58 ml | 3.16 ml |
5 mM | 0.063 ml | 0.316 ml | 0.632 ml |