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CP-466722

Catalog No. S2245 Name Selleck Chemicals
CAS Number 1080622-86-1 Website http://www.selleckchem.com
M. F. C17H15N7O2 Telephone (877) 796-6397
M. W. 349.3467 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 73109

SYNONYMS

IUPAC name
1-(6,7-dimethoxyquinazolin-4-yl)-3-(pyridin-2-yl)-1H-1,2,4-triazol-5-amine
IUPAC Traditional name
2-(6,7-dimethoxyquinazolin-4-yl)-5-(pyridin-2-yl)-1,2,4-triazol-3-amine
Synonyms
CP466722

DATABASE IDS

CAS Number 1080622-86-1

PROPERTIES

Target ATM
Salt Data Free Base
Storage Condition -20°C

DETAILS

Description (English)
Research Area
Description Cancer
Biological Activity
Description CP-466722 is an potent and reversible ATM inhibitor.
Targets ATM
IC50
In Vitro In vitro, CP-466722 is identified as a potential inhibitor to decrease the activity of purified ATM kinase to phosphorylate GST-p53(1–101) substrate. In addition, CP-466722 also shows the inhibitory activities against abl and src kinases. [1] In HeLa cells, CP-466722 at doses of 6μM, results in the inhibition in ATM-dependent phosphorylation by reversibly inhibiting ionizing radiation (IR)-induced ATM kinase activity. Besides, ATM-dependent p53 induction is also inhibited by CP-466722 in MCF-7 human breast cancer cells and primary and immortalized diploid human fibroblasts. [1] In response to IR, CP-466722 increased proportion of cells with G2/M DNA content and reduces proportion of cells with G1-phase DNA content in HeLa cells. [1] Transient exposure to CP-466722 for a period of 4 hours sensitizes HeLa cells to IR without affecting cell plating nor cell viability. [1]
In Vivo
Clinical Trials
Features
Protocol
Cell Assay [1]
Cell Lines HeLa and A-T
Concentrations 0-6 μM
Incubation Time 4 hours
Methods HeLa or A-T (GM02052 expressing hTERT) cells are plated in triplicate and incubated for 24 hours. Cells are pre-treated: DMSO, CP466722 or KU55933 prior to IR (0-10Gy). Cells are incubated for 4 hours following IR before media is removed, cells washed (PBS), trypsinsed, counted and re-plated (2000 cells/plate, 10 cm plates) in the absence of drug and incubated for 10 days. Prior to colony counting, cells are washed (PBS), stained (PBS, 0.0037%v/v-formaldehyde, 0.1%w/v-crystal violet), rinsed (dH2O) and dried. Defined populations (>50 cells) are counted as one surviving colony, data are calculated as percentage surviving colonies relative to control plates +/? SE.
References
[1] Rainey MD, et al. Cancer Res, 2008, 68(18), 7466-7474.