Chemical Structure : EXEL-1855
CAS No.:
3086824-79-2
EXEL-1855
(EXEL1855)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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618.56
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Formula
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C26H29F7N8O2
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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)-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
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References
1. Gonciarz RL, et al. J Med Chem. 2026 Oct 8;69(19):22637-22656.
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