Catalog No.: PC-25509Not For Human Use, Lab Use Only.
Tarloxotinib (TH-4000) is a hypoxia-activated pan-HER inhibitor, generates the active form TH-4000Effector (TH-4000E) under hypoxic condition, TH-4000E selectively inhibits EGFR, HER2 and HER4 with IC50 of <1 nM.
Tarloxotinib (TH-4000) is a hypoxia-activated pan-HER inhibitor, generates the active form TH-4000Effector (TH-4000E) under hypoxic condition, TH-4000E selectively inhibits EGFR, HER2 and HER4 with IC50 of <1 nM. TH-4000E has a highly selective inhibitory effect on HER2+ breast cancer cells, shows IC50 of 8.84 nM, 13.14 nM, 108.92 nM and 126.20 nM for HER2+ breast cancer cells BT-474, SK-BR-3, HCC-1954 and JIMT-1 respectively. TH-4000E showed highest selectivity to EGFR, HER2 and HER4 among 217 kinases, with IC50 of <1 nM. TH-4000E inhibits phosphorylation of HER family proteins in HER2+ breast cancer cells. TH-4000E induces cellular apoptosis in HER2+ breast cancer cells, through a ROS-dependent manner. Tarloxotinib (TH-4000) (50 mg/kg per week by intraperitoneal injection) inhibited tumor growth in a xenograft model.
