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ZL-2201

Chemical Structure : ZL-2201

CAS No.: 2646592-18-7

ZL-2201 (ZL2201)

Catalog No.: PC-21128Not For Human Use, Lab Use Only.

ZL-2201 (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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ZL-2201 (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.

Physicochemical Properties

M.Wt 407.44
Formula C19H21N9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

9-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-7-methyl-2-((7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino)-7,9-dihydro-8H-purin-8-one

References

1. Shruti Lal, et al. Cancer Res Commun. 2023 Sep 1;3(9):1731-1742.

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