2. Academic Validation
  3. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model

CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model

  • ACS Med Chem Lett. 2016 Jun 10;7(8):768-73. doi: 10.1021/acsmedchemlett.6b00149.
Andrew D Cansfield 1,  Tammy Ladduwahetty 1,  Mihiro Sunose 1,  Katie Ellard 1,  Rosemary Lynch 1,  Anthea L Newton 1,  Ann Lewis 1,  Gavin Bennett 1,  Nico Zinn 2,  Douglas W Thomson 2,  Anne J Rüger 2,  John T Feutrill 1,  Oliver Rausch 1,  Alan P Watt 1,  Giovanna Bergamini 2
Affiliations

Affiliations

  • 1 Cellzome Ltd , Chesterford Research Park, Saffron Waldon, CB10 1XL, United Kingdom.
  • 2 Cellzome AG , Meyerhofstraße 1, 69117 Heidelberg, Germany.
PMID: 27563401 DOI: 10.1021/acsmedchemlett.6b00149
Abstract

CZ415, a potent ATP-competitive mTOR Inhibitor with unprecedented selectivity over any other kinase is described. In addition to a comprehensive characterization of its activities in vitro, in vitro ADME, and in vivo pharmacokinetic data are reported. The suitability of this inhibitor for studying in vivo mTOR biology is demonstrated in a mechanistic mouse model monitoring mTOR proximal downstream phosphorylation signaling. Furthermore, the compound reported here is the first ATP-competitive mTOR Inhibitor described to show efficacy in a semitherapeutic collagen induced arthritis (CIA) mouse model.

Keywords

collagen induced arthritis model; inflammation; kinase inhibitor; mTOR.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-100222
    98.74%, mTOR Inhibitor