Tarloxotinib bromide

Research use only, not for human use.

Tarloxotinib bromide is an irreversible inhibitor of EGFR/HER2.

Tarloxotinib bromide is an irreversible inhibitor of EGFR/HER2.(In Vitro):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.(In Vivo):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.

TH-4000

Angiogenesis

EGFR

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1636180-98-7

681.8

C24H24Br2ClN9O3

>98% (HPLC)

——

[Br-].Cn1cnc(c1C[N+](C)(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(Cl)c(Br)c3)ncnc2cn1)[N+]([O-])=O

——

(-20℃)

With Ice Pack

≥ 2 years