ZL-2201 mesylate | DNA-PK inhibitor | Probechem Biochemicals

Chemical Structure : ZL-2201 mesylate

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ZL-2201 mesylate (ZL2201 mesylate)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	503.54
分子式	C20H25N9O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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)

参考文献

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

ZL-2201 mesylate (ZL2201 mesylate)

生物&药学活性

物理化学性质&存储条件

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ZL-2201 mesylate (ZL2201 mesylate)

生物&药学活性

物理化学性质&存储条件

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