MedChemExpress - Model CCT365623 hydrochloride -2126136-98-7

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].

CCT365623 hydrochloride

MCE China：CCT365623 hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-124674A

CAS：2126136-98-7

Purity：98.07%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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 T1/2PO of 0.6 h and F% (oral bioavailability) of 45%[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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CCT365623 hydrochloride Related Antibodies Western Blot Analysis[1] Cell Line: MDA-MB-231 cells.

References：

[1]. Tang H, et al. Author Correction: Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface. Nat Commun. 2019 Jul 18;10(1):3151. [Content Brief]

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MedChemExpress - Model CCT365623 hydrochloride -2126136-98-7

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CCT365623 hydrochloride