FLYNN, DANIEL L.,KAUFMAN, MICHAEL D.,SMITH, BRYAN D.
申请号:
CA2971874
公开号:
CA2971874A1
申请日:
2015.10.14
申请国别(地区):
CA
年份:
2016
代理人:
摘要:
It has been shown that Compound 1 unexpectedly and potently inhibits TRK kinases, including all three forms of TRK: NTRKl, NTRK2, and NTRK3. Additionally it has been shown that Compound 1 potently inhibits oncogenic mutated forms of TRK kinases, including fusion proteins. By way of exemplification, Compound 1 potently inhibits the NTRKl oncogenic fusion protein TPM3/NTRK1 in cellular assays. Compound 1 inhibits TRK kinase mediated tumor growth in vivo in a TPM3/NTRK1 xenograft model.