Tarloxotinib bromide 是一种不可逆的 EGFR/HER2 抑制剂。

Tarloxotinib bromide is an irreversible inhibitor of EGFR/HER2.

Tarloxotinib bromide is metabolized efficiently under hypoxia using a panel of human NSCLC cell lines (rate of TKI release 0.4-2.1 nM/hr/106 cells), a process that is inhibited by oxygen (TKI release<0.002 nM/hr/106 cells). Cellular anti-proliferative and receptor phosphorylation assays demonstrate a 14-80 fold reduction of Tarloxotinib bromide activity relative to TKI. Using PC9 tumors, hyperbaric oxygen breathing suppresse release of TKI from Tarloxotinib bromide by >80% (538 vs 99 nM/kg; p<0.01) compared to air breathing controls[1].

Tarloxotinib bromide treatment regresses the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo[2].

1636180-98-7

C24H24Br2ClN9O3

681.77

TH-4000

DMSO:33 mg/mL (48.40 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years