1429639-50-8 Usage
Description
CZ415 is an inhibitor of mammalian target of rapamycin (mTOR; Kd = 6.3 nM), which is 1,000-fold selective for mTOR over a panel of 285 kinases. It effectively inhibits phosphorylation of S6 ribosomal protein (S6RP) and Akt in HEK293T cells (IC50s = 14.5 and 14.8 nM, respectively) and IFN-γ secretion in IL-2, anti-CD3, and anti-CD28 antibody-stimulated human whole blood (IC50 = 226 nM).
Uses
Used in Pharmaceutical Industry:
CZ415 is used as a selective and potent ATP-competitive mTOR inhibitor for demonstrating in vivo efficacy in a semitherapeutic collagen-induced arthritis (CIA) mouse model. Its ability to inhibit mTOR activity and reduce tumor growth makes it a promising candidate for the development of targeted therapies in various cancer types.
Used in Arthritis Treatment:
CZ415 is used as an anti-inflammatory agent for reducing fore paw joint erythema and swelling in a mouse model of collagen-induced arthritis. Its efficacy in this model suggests potential applications in the treatment of inflammatory conditions and autoimmune diseases.
Used in Oncology:
CZ415 is used as an anticancer agent for inhibiting intratumor mTOR activity and reducing tumor growth in an OCC-1 oral cavity carcinoma mouse xenograft model when administered at a dose of 20 mg/kg. Its role in modulating key signaling pathways involved in cancer progression highlights its potential as a therapeutic agent in oncology.
Check Digit Verification of cas no
The CAS Registry Mumber 1429639-50-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,2,9,6,3 and 9 respectively; the second part has 2 digits, 5 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1429639-50:
(9*1)+(8*4)+(7*2)+(6*9)+(5*6)+(4*3)+(3*9)+(2*5)+(1*0)=188
188 % 10 = 8
So 1429639-50-8 is a valid CAS Registry Number.
1429639-50-8Relevant articles and documents
CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model
Cansfield, Andrew D.,Ladduwahetty, Tammy,Sunose, Mihiro,Ellard, Katie,Lynch, Rosemary,Newton, Anthea L.,Lewis, Ann,Bennett, Gavin,Zinn, Nico,Thomson, Douglas W.,Rüger, Anne J.,Feutrill, John T.,Rausch, Oliver,Watt, Alan P.,Bergamini, Giovanna
, p. 768 - 773 (2016/08/24)
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.
