WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 571057
Description: QC6352 is a potent KDM4 family inhibitor that is efficacious in breast and colon cancer PDX models. QC6352 demonstrated an IC50 of 5 nM in BR0869f after a 5-day incubation, and an IC50 of 13 nM in the SU60 model. as excellent physical properties and drug-like characteristics. QC6352 showed favorable in vivo efficacy in a breast cancer PDX model and reduced the tumor initiating cell populations, which are associated with resistance to chemotherapy treatments.
MedKoo Cat#: 571057
Chemical Formula: C24H25N3O2
Exact Mass: 387.1947
Molecular Weight: 387.483
Elemental Analysis: C, 74.39; H, 6.50; N, 10.84; O, 8.26
Synonym: QC6352; QC-6352; QC 6352.
IUPAC/Chemical Name: (R)-3-(((6-(methyl(phenyl)amino)-1,2,3,4-tetrahydronaphthalen-1-yl)methyl)amino)isonicotinic acid
InChi Key: XSMABFRQESMONQ-SFHVURJKSA-N
InChi Code: InChI=1S/C24H25N3O2/c1-27(19-8-3-2-4-9-19)20-10-11-21-17(14-20)6-5-7-18(21)15-26-23-16-25-13-12-22(23)24(28)29/h2-4,8-14,16,18,26H,5-7,15H2,1H3,(H,28,29)/t18-/m0/s1
SMILES Code: O=C(O)C1=CC=NC=C1NC[C@@H]2CCCC3=C2C=CC(N(C)C4=CC=CC=C4)=C3
KDM4 genes and proteins are overexpressed in numerous tumor types including breast, colorectal, pancreatic, lymphoma, and gastric cancers. KDM4 family members also play an important role in the epigenetic regulation of embryonic stem cell identity.
Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models
ACS Med. Chem. Lett. DOI: 10.1021/acsmedchemlett.7b00220
Young K. Chen,† Tiziana Bonaldi,# Alessandro Cuomo,# Joselyn R. Del Rosario,† David J. Hosfield,§
Toufike Kanouni,† Shih-chu Kao,‡,● Chon Lai,† Neethan A. Lobo,‡ Jennifer Matuszkiewicz,†
Andrew McGeehan,‡ Shawn M. O’Connell,†,▲ Lihong Shi,† Jeffrey A. Stafford,†,■ Ryan K. Stansfield,†,■
James M. Veal,†,■ Michael S. Weiss,‡,□ Natalie Y. Yuen,‡ and Michael B. Wallace*,†
†Celgene Quanticel Research, 10300 Campus Point Drive, Suite 100, San Diego, California 92121, United States
‡Celgene Quanticel Research, 1500 Owens Street, Suite 500, San Francisco, California 94158, United States
#Department of Experimental Oncology, European Institute of Oncology, Via Adamello 16, 20139 Milano, Italy
§Ben May Department for Cancer Research, University of Chicago, 929 East 57th Street, Chicago, Illinois 60637, United States