APL-4098 (APL4098)

Chemical Structure : APL-4098

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	434.83
分子式	C17H12ClFN6O3S
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	N-(4-((2-aminopyrimidin-5-yl)ethynyl)-3-fluoropyridin-2-yl)-5-chloro-2-methoxypyridine-3-sulfonamide

参考文献

1. Román-Trufero M, et al. Clin Cancer Res. 2026 Feb 23. doi: 10.1158/1078-0432.CCR-25-1444.

APL-4098 (APL4098)

生物&药学活性

物理化学性质&存储条件

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APL-4098 (APL4098)

生物&药学活性

物理化学性质&存储条件

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