TAK-165 can inhibit HT1376, UMUC3, T24 (bladder), ACHN (kidney), DU145, LNCaP, LN-REC4 (prostate) cell lines, which are observed HER2 expression, with IC50 from 0.09 to greater than 25 micromol/L. The prostate cancer cell lines are all sensitive to mubritinib (TAK 165).Mubritinib (TAK 165) can inhibit prostate cancer cell lines with IC50 from 0.053to 4.62 micromol/L.
In vivo
In the xenograft model, treatment with TAK-165 significantly inhibited growth of UMUC-3, ACHN, and LN-REC4. The antitumor effect (T/C [%]=growth of TAK-165 treated tumor/average growth of control tumorx100) after 14 days treatment were 22.9%, 26.0%, and 26.5% in UMUC3, ACHN and LN-REC4, respectively.