Catalog Number: 5280
Chemical Name: 2-[2-[(6-Methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy]ethanol
Biological Activity
Potent MTH1 inhibitor (Kd = 49 nM). Inhibits Ras-induced malignant transformation and increases α-actin promoter-driven CAT activity in Ras-transformed cells. Has no effect on Ras-induced ERK and JNK activation. Inhibits Ras-induced membrane ruffling in REF-52 fibroblasts and blocks anchorage-independent growth of Ras-transformed tumor cell lines. Also induces DNA damage in SW480 colon cancer cells.
Technical Data
  • M.Wt:
    316.35
  • Formula:
    C16H20N4O3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    171927-40-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.
    Huber KV, Salah E, Radic B et al.
    Nature
  2. SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway.
    Walsh et al.
    Oncogene, 1997;15:2553
  3. SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway.
    Kumar et al.
    Ann.N.Y.Acad.Sci., 1999;886:122

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