Chemical Structure : FORX-428
CAS No.:
2922789-15-7
FORX-428
(FORX428 )
Catalog No.: PC-26761Not For Human Use, Lab Use Only.
FORX-428 (FORX428) is a highly potent, selective and orally bioavailable PARG inhibitor with IC50 of 0.29 nM and 0.25 nM for PARG WT human and PARG WT mouse respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
FORX-428 (FORX428) is a highly potent, selective and orally bioavailable PARG inhibitor with IC50 of 0.29 nM and 0.25 nM for PARG WT human and PARG WT mouse respectively.
FORX-428 shows high binding affinitt to PARG with SPR Kd of 0.09 nM.
FORX-428 shows selective reduction of viability in a panel of cancer cell lines, RMUG-S (ovarian, IC50=0.6 nM), MDA-MB-436 (breast, IC50=19 nM).
FORX-428 induces a dose-dependent accumulation of PAR chains in vivo which constitutes a tractable target engagement biomarker for clinical exploration.
FORX-428 demonstrates compelling anti-tumor efficacy as single agent in several xenograft models (breast & ovarian cancer) with excellent tolerability.
Physicochemical Properties
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M.Wt
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497.58
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Formula
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C20H25F2N7O2S2
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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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3-(5-(Difluoromethyl)-1,3,4-thiadiazol-2-yl)-8-((3S,5S)-3,5-dimethylpiperazin-1-yl)-N-(1-methylcyclopropyl)imidazo[1,5-a]pyridine-6-sulfonamide
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References
1. Frank Tadashi. Zenke, et al. Mol Cancer Ther (2025) 24 (10_Supplement): B022.
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