Chemical Structure : ZL-2201 mesylate
CAS No.:
2865115-39-3
ZL-2201 mesylate
(ZL2201 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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
503.54
|
|
Formula
|
C20H25N9O5S
|
|
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
|
8H-Purin-8-one, 7,9-dihydro-7-methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-, methanesulfonate (1:1)
|
References
1. Shruti Lal, et al. Cancer Res Commun. 2023 Sep 1;3(9):1731-1742.
Contact Us
sales@probechem.com
