MedChemExpress - Model XRD-0394 -2595308-10-2
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XRD-0394
MCE China：XRD-0394
Brand：MedChemExpress (MCE)
Cat. No.HY-162472
CAS：2595308-10-2
Purity：98.54%
Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro.
In Vitro：XRD-0394 (20 nM, 100 nM, 500 nM, 1000 nM; pretreated with 30 minutes and then irradiated with 0-10 Gy for 1 hour) inhibits phosphorylation by ATM and DNA-PK kinases, but not structurally related kinases in MCF7 human tumor cells[1].
In Vivo：XRD-0394 (3-10 mg/kg) via oral gavage 45 minutes prior to focal radiotherapy of 0 or 10 Gy and tumors are harvested for target inhibition assessment 1 hour after irradiation, XRD-0394 inhibits the activities of both DNA-PK and ATM kinases in tumors in vivo[1]. Pharmacokinetic analyses show that 10 mg/kg XRD-0394 (oral gavage) resulted in plasma concentration of 840-1,125 ng/mL (1.6-2.1 mM) for 4 hours before declining to undetectable levels by 24 hours in mice[1].
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References：
[1]. Gilmer T M, et al. A novel dual ATM/DNA-PK inhibitor, XRD-0394, potently radiosensitizes and potentiates PARP and topoisomerase I inhibitors[J]. Molecular Cancer Therapeutics, 2024. [Content Brief]
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