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Chemical Structure : AZ1366
Catalog No.: PC-49491Not For Human Use, Lab Use Only.
AZ1366 (AZ-1366) is a potent and selective inhibitor of TNSK1/2 with IC50 of 7 nM (TNKS1), also inhibits PARP1 with IC50 of 6 nM, shows Wnt pathway inhibition in DLD-1 cells (IC50<3 nM).
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AZ1366 (AZ-1366) is a potent and selective inhibitor of TNSK1/2 with IC50 of 7 nM (TNKS1), also inhibits PARP1 with IC50 of 6 nM, shows Wnt pathway inhibition in DLD-1 cells (IC50<3 nM).
AZ1366 showed qualitatively stronger and longer lasting stabilization of Axin2, TNKS1, and TNKS2 at lower concentrations compared to XAV939 in DLD-1 cells.
AZ1366 synergistically suppresses NSCLC proliferation when combined with EGFR inhibitor gefitinib, exerts antiproliferative effects through inhibition of the canonical Wnt pathway.
AZ1366 inhibits basal and Wnt3a-activated β-catenin-dependent transcription in HCCC4006.
AZ1366 provided increased tumor control and improved survival in mice harboring Wnt-responsive tumors when combined with EGFR inhibitors.
| M.Wt | 416.48 | |
| Formula | C24H24N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Scarborough HA, et al. Clin Cancer Res. 2017 Mar 15;23(6):1531-1541.
2. Quackenbush KS, et al. Oncotarget. 2016 May 10;7(19):28273-85.
3. Johannes JW,et al. ACS medicinal chemistry letters. 2015;6(3):254–59.
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