CCT365623 (hydrochloride)

CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC₅₀ of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties^[1]. IC50 & Target: IC50: 0.89 μM (LOX)^[1]. In Vitro: CCT365623 inhibits LOX at ~5 μM in the biosensor system^[1].
CCT365623 (0-40 μM) concentration-dependently decreases the protein levels of surface EGFR^[1].
CCT365623 (5 μM) decreases the protein levels of pY1068 EGFR, pAKT and MATN2, and increases the protein levels of pSMAD2^[1].
CCT365623 disrupts HTRA1 multimerization, activates TGFβ1 signalling, suppresses MATN2 expression, suppresses EGFR surface retention, and suppresses EGFR signalling^[1].
In Vivo: CCT365623 displays good stability in mouse liver microsomes and does not inhibit the cardiac potassium channel hERG^[1].
CCT365623 (70 mg/kg, oral gavage per day) significantly delays the development of the primary tumors and also suppresses metastatic lung burden in the animals. CCT365623 disrupts EGFR cell surface retention and delays the growth of primary and metastatic tumor cell^[1].
CCT365623 exhibits a T_1/2PO of 0.6 h and F% (oral bioavailability) of 45%^[1].