Chemical Structure : WSD0628
CAS No.:
2765448-96-0
WSD0628
(WSD-0628)
Catalog No.: PC-24377Not For Human Use, Lab Use Only.
WSD0628 (WSD-0628) is a potent, selective, orally bioavailable and CNS penetrant ATM inhibitor, potently inhibits ATM-mediated phosphorylation of the DNA damage response protein KAP1 in MCF-7 cells with IC50 of 0.42 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
WSD0628 (WSD-0628) is a potent, selective, orally bioavailable and CNS penetrant ATM inhibitor, potently inhibits ATM-mediated phosphorylation of the DNA damage response protein KAP1 in MCF-7 cells with IC50 of 0.42 nM.
WSD0628 is much less potent inhibition of the related kinases ATR (phosphorylation of CHK1, IC50 742nM) or DNA-PKcs (auto-phosphorylation of DNA-PK, IC50 169nM) in HT29 cells.
WSD-0628 (30 nM) potently inhibited RT-induced phospho-KAP1 and robustly reduced clonogenic survival by 5-fold when combined with 5 Gy irradiation in U251 GBM cells.
WSD0628 is orally bioavailable and CNS penetrant without efflux transporter liability.
Physicochemical Properties
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M.Wt
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439.47
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Formula
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C23H23F2N5O2
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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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(R)-1-(3,3-Difluoro-1-methylpiperidin-4-yl)-8-(6-methoxypyridin-3-yl)-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one
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References
1. Rathi S, et al. J Pharmacol Exp Ther. 2024 Jul 18;390(2):260-275.
2. Tuma, A. M. et al. Abstract 3305: WSD-0628, a novel brain penetrant ATM inhibitor, radiosensitizes GBM and melanoma patient derived xenografts. Cancer Res. 2022, 82, 3305– 3305.
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