CCT365623 is a Lysyl oxidase inhibitor. CCT365623 disrupts EGFR cell surface retention and delays the growth of primary and metastatic tumour cells in vivo. LOX regulates EGFR cell surface retention to drive tumour progression.
CAS Number: 2126136-98-7
Molecular Weight: 443.99
Chemical Name: C-[5-(5-Methanesulfonyl-biphenyl-3-sulfonyl)-thiophen-2-yl]-methylamine Hydrochloride
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
CCT365623 inhibits LOX at ~5 μM in the biosensor system. CCT365623 (0-40 μM) concentration-dependently decreases the protein levels of surface EGFR. CCT365623 (5 μM) decreases the protein levels of pY1068 EGFR, pAKT and MATN2, and increases the protein levels of pSMAD2. CCT365623 disrupts HTRA1 multimerization, activates TGFβ1 signalling, suppresses MATN2 expression, suppresses EGFR surface retention, and suppresses EGFR signalling.
- Tang H, Leung L, Saturno G, Viros A, Smith D, Di Leva G, Morrison E, Niculescu-Duvaz D, Lopes F, Johnson L, Dhomen N, Springer C, Marais R. Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface. Nat Commun. 2017 Apr 18;8:14909. doi: 10.1038/ncomms14909. PubMed PMID: 28416796; PubMed Central PMCID: PMC5399287.
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