1645286-58-3
Chemical Structure
AZ1366
- CAS No.: 1645286-58-3
- Formula:C24H24N4O3
- Molecular Weight:416.48
IUPAC Name: 8-(hydroxymethyl)-2-(4-(6-((2-methoxyethyl)amino)-4-methylpyridin-3-yl)phenyl)quinazolin-4(1H)-one
InChIKey: PLGIKHVPQHSSON-UHFFFAOYSA-N
SMILES: O=C1N=C(NC=2C1=CC=CC2CO)C=3C=CC(=CC3)C=4C=NC(=CC4C)NCCOC
Biological Activity: AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer[1][2].
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AZ1366 | AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer. | |||||||||||||||||||||
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- [1]. Quackenbush KS, et al. The novel tankyrase inhibitor (AZ1366) enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Oncotarget. 2016;7(19):28273-28285. [Content Brief]
- [2]. Scarborough HA, et al. AZ1366: An Inhibitor of Tankyrase and the Canonical Wnt Pathway that Limits the Persistence of Non-Small Cell Lung Cancer Cells Following EGFR Inhibition. Clin Cancer Res. 2017;23(6):1531-1541. [Content Brief]
Keywords
