EXEL-1855 | PLK4 inhibitor | Probechem Biochemicals

Chemical Structure : EXEL-1855

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EXEL-1855 (EXEL1855)

货号: PC-28563Not For Human Use, Lab Use Only.

EXEL-1855 is a potent, selective and orally bioavailable Polo-like kinase 4 (PLK4) inhibitor with IC50 of 7.7 nM in ADPGlo assays and EC50 of 33 nM in Nano BRET assays.

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生物&药学活性

EXEL-1855 is a potent, selective and orally bioavailable Polo-like kinase 4 (PLK4) inhibitor with IC50 of 7.7 nM in ADPGlo assays and EC50 of 33 nM in Nano BRET assays.
EXEL-1855 displays excellent selectivity against an external panel of kinases, inhibiting only 7 out of 418 kinases greater than 80% at 1 μM in the Eurofins KinaseProfiler screen.
EXEL-1855 shows excellent CHP-134 potency (cell viability EC50=12 nM) and AURKB selectivity.
EXEL-1855 (10, 30, and 100 mg/kg, 0.5% methylcellulose/0.5% Tween 80, oral QD) showed robust efficacy in CHP-134 neuroblastoma mouse xenograft model.

物理化学性质&存储条件

分子量	618.56
分子式	C26H29F7N8O2
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	(R)-N-(3-(1-(2-Fluoro-2-methylpropyl)-3-(3-(trifluoromethyl)azetidin-1-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)-1H-pyrazol-4-yl)-7-hydroxy-7-(trifluoromethyl)-4-azaspiro[2.5]octane-4-carboxamide

参考文献

1. Gonciarz RL, et al. J Med Chem. 2026 Oct 8;69(19):22637-22656.

EXEL-1855 (EXEL1855)

生物&药学活性

物理化学性质&存储条件

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EXEL-1855 (EXEL1855)

生物&药学活性

物理化学性质&存储条件

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