Chemical Name: N-[5-(2,3-Dihydro-1,4-benzodioxine-6-carbonylamino)-2-methylphenyl]-2-(2-pyrrolidin-1-ylethoxy)quinoline-6-carboxamide
HSF stress pathway inhibitor
Molekulargewicht:
552.63
Reinheit:
98% by HPLC NMR (Conforms)
Formulierung:
Off-white/beige solid
CAS Nummer:
[1693731-40-6]
Formel:
C32H32N4O5
Anwendungsbeschreibung:
Inhibitor of the Heat Shock Transcription Factor 1 (HSF1) stress pathway (IC50 = 19 nM Inhibition HSF-1 mediated HSP72 induction, IC50 = 40 nM HSPA1A induction).1 It displayed efficacy in a human ovarian carcinoma xenograft mouse model (SK-OV 3 cells) and inhibited migration of WM266.4 melanoma cells 100 nM. CCT251236 showed high affinity for the protein pirin (Ki = 28 nM), but this target was not shown conclusively to be the cause of the anticancer activity. It also showed efficacy in vitro against primary patient-derived myeloma cells and H929 human myeloma xenograft models.2
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