CCT365623 HCl

Cas：2126136-98-7

Product Information：

CCT365623 HCl is an inhibitor of Lysyl oxidase (LOX).

Chemical Formula: C18H18ClNO4S3

Exact Mass:

Molecular Weight: 443.98

Elemental Analysis: C, 48.70; H, 4.09; Cl, 7.98; N, 3.15; O, 14.41; S, 21.66

Related CAS #: 2126134-01-6 (free base)   2126136-98-7 (HCl)  

Chemical Name: C-[5-(5-Methanesulfonyl-biphenyl-3-sulfonyl)-thiophen-2-yl]-methylamine Hydrochloride

InChi Key:

MKBRQENFVVWIGU-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H17NO4S3.ClH/c1-25(20,21)16-9-14(13-5-3-2-4-6-13)10-17(11-16)26(22,23)18-8-7-15(12-19)24-18;/h2-11H,12,19H2,1H3;1H

SMILES Code: NCC1=CC=C(S(=O)(C2=CC(C3=CC=CC=C3)=CC(S(=O)(C)=O)=C2)=O)S1.[H]Cl

Technical Data：

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

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.

In Vivo：

CCT365623 displays good stability in mouse liver microsomes and does not inhibit the cardiac potassium channel hERG.

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.

CCT365623 exhibits a T1/2PO of 0.6 h and F% (oral bioavailability) of 45%.

References：

1. 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.

Products are for research use only. Not for human use.