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Chemical Structure : ZL-2201 mesylate
Catalog No.: PC-21129Not For Human Use, Lab Use Only.
ZL-2201 mesylate (ZL2201) is a highly potent, selective and orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 of 1.1 nM.
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ZL-2201 mesylate (ZL2201) is a highly potent, selective and orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 of 1.1 nM.
ZL-2201 shows no significant activities against human mTOR, ATM, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ PI3-kinases (all IC50 >1000 nM).
ZL-2201 exhibits antiproliferative activity against ATM-deficient NSCLC cell lines (H1373, H23, H522, H1395, H1703) with IC50 of 3.98-12.2 uM, selectively inhibits DNA-PK autophosphorylation at Ser2056.
ZL-2201 robustly inhibits NHEJ-mediated repair of exogenous DNA damage resulting in increased G2–M arrest and apoptosis in vitro.
ZL-2201 (60 mg/kg) inhibits DNA-PK autophosphorylation and exhibits potent antitumor efficacy in vivo of NCI-H1703 xenografts.
ZL-2201 could synergy with various DNA-damaging agents, significantly augments antitumor activity of DSB-inducing agents doxorubicin and IR.
| M.Wt | 503.54 | |
| Formula | C20H25N9O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Shruti Lal, et al. Cancer Res Commun. 2023 Sep 1;3(9):1731-1742.
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