Chemical Structure : APL-4098
CAS No.:
2752441-61-3
APL-4098
(APL4098)
Catalog No.: PC-26070Not For Human Use, Lab Use Only.
APL-4098 is a potent, selective, ATP-binding site competitive GCN2 inhibitor with Ki of 4.39 nM in TR-FRET assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
APL-4098 is a potent, selective, ATP-binding site competitive GCN2 inhibitor with Ki of 4.39 nM in TR-FRET assays.
APL-4098 inhibits eIF2α phosphorylation in a concentration-dependent manner with IC50 of 50.8 nM in HTRF assays in the presence of borrelidin.
APL-4098 induces cell death in patient derived AML cells.
APL-4098 impairs mitochondrial respiration and triggers the mitochondrial unfolded protein response (UPR).
APL-4098 (0.5 and 5 mg/kg, oral) shows anti-tumor activity in AML CDX model.
Combined APL-4098 and venetoclax reduce leukemic burden and depletes LSCs in vivo.
Physicochemical Properties
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M.Wt
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434.83
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Formula
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C17H12ClFN6O3S
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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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N-(4-((2-aminopyrimidin-5-yl)ethynyl)-3-fluoropyridin-2-yl)-5-chloro-2-methoxypyridine-3-sulfonamide
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References
1. Román-Trufero M, et al. Clin Cancer Res. 2026 Feb 23. doi: 10.1158/1078-0432.CCR-25-1444.
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