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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ATM/ATR-XRD-0394 hydrochloride
XRD-0394 hydrochloride

Chemical Structure : XRD-0394 hydrochloride

CAS No.: 2595308-11-3

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XRD-0394 hydrochloride (XRD0394 hydrochloride)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 564.07
分子式 C26H31ClFN5O4S
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

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 hydrochloride

参考文献

1. Gilmer TM, et al. Mol Cancer Ther. 2024 Apr 8. doi: 10.1158/1535-7163.MCT-23-0890.

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