Chemical Name: 1-(1-Methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Biological ActivityPotent RET inhibitor (IC50 = 8 nM). Also exhibits inhibitory activity at EphA1, FGFR1, Flt4, Lck and Yes. Inhibits proliferation of HCT 116 and TPC1 cells in vitro. Cell permeable.
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.
Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors.
Dinér et al.
Design, synthesis and characterization of a highly effective inhibitor for analog-sensitive (as) kinases.
Klein et al.
PLoS ONE, 2011;6:e20789
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