FORX-428 (FORX428) | PARG inhibitor | Probechem Biochemicals

Chemical Structure : FORX-428

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FORX-428 (FORX428 )

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	497.58
分子式	C20H25F2N7O2S2
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	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

参考文献

1. Frank Tadashi. Zenke, et al. Mol Cancer Ther (2025) 24 (10_Supplement): B022.

FORX-428 (FORX428 )

生物&药学活性

物理化学性质&存储条件

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FORX-428 (FORX428 )

生物&药学活性

物理化学性质&存储条件

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