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This Letter describes the lead discovery, optimization, and biological characterization of a series of substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as potent inhibitors of IGF1R, EGFR, and ErbB2. The leading compound 11 showed an IGF1R IC 50 of 12nM, an EGFR (L858R) IC 50 of 31nM, and an ErbB2 IC 50 of 11nM, potent activity in cellular functional and anti-proliferation...
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