WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H571057
CAS#: 1851373-36-8
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.
Hodoodo Cat#: H571057
Name: QC6352
CAS#: 1851373-36-8
Chemical Formula: C24H25N3O2
Exact Mass: 387.19
Molecular Weight: 387.483
Elemental Analysis: C, 74.39; H, 6.50; N, 10.84; O, 8.26
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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
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: >2 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
More Info: 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.
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 387.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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