Chemical Structure : XRD-0394
CAS No.:
2595308-10-2
XRD-0394
(XRD0394)
Catalog No.: PC-22113Not For Human Use, Lab Use Only.
XRD-0394 (XRD0394) is a potent and specific 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
XRD-0394 (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.
Physicochemical Properties
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M.Wt
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527.62
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Formula
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C26H30FN5O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(5-(7'-fluoro-3'-methyl-2'-oxo-2',3'-dihydrospiro[cyclobutane-1,1'-pyrrolo[2,3-c]quinolin]-8'-yl)-2-(2-(isopropylamino)ethoxy)pyridin-3-yl)methanesulfonamide
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References
1. Gilmer TM, et al. Mol Cancer Ther. 2024 Apr 8. doi: 10.1158/1535-7163.MCT-23-0890.
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