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Chemical Structure : XRD-0394 hydrochloride
Catalog No.: PC-22114Not For Human Use, Lab Use Only.
XRD-0394 hydrochloride (XRD0394) is a potent, specific, orally bioavailable dual inhibitor of DNA damage-response kinases ATM and DNA-PK with IC50 of 0.39 and 0.89 nM, respectively.
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XRD-0394 hydrochloride (XRD0394) is a potent, specific, orally bioavailable dual inhibitor of DNA damage-response kinases ATM and DNA-PK with IC50 of 0.39 and 0.89 nM, respectively.
XRD-0394 is >100-fold selective for ATM and DNA-PK versus mTOR, PI3Kβ, ATR and SMG-1 and > 40-fold selective versus PI3Kγ and PI3Kδ, and 14-fold selective versus PI3Kα.
XRD-0394 inhibits phosphorylation by ATM and DNA-PK kinases, but not structurally related kinases, in human tumor cell.
XRD-0394 shows both significantly greater radiosensitization and less cellular toxicity in the absence of IR when compared to a specific ATR inhibitor, RP3500.
XRD-0394 also potentiates the effectiveness of topoisomerase I inhibitors in vitro.
XRD-0394 shows single agent activity and synergy in combination with PARP inhibitors in cells lacking BRCA1/2.
| M.Wt | 564.07 | |
| Formula | C26H31ClFN5O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Gilmer TM, et al. Mol Cancer Ther. 2024 Apr 8. doi: 10.1158/1535-7163.MCT-23-0890.
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