EOS301984 (EOS-984) | ENT1 inhibitor | Probechem Biochemicals

Chemical Structure : EOS301984

CAS No.: 2724937-55-5

EOS301984 (EOS984, EOS-984, EOS-301984)

Catalog No.: PC-23833Not For Human Use, Lab Use Only.

EOS301984 (EOS-984) is a potent, selective equilibrative nucleoside transporter 1 (ENT1) antagonist with IC50 of 339.6 nM (human ENT1), 150-fold selectivity for ENT1 versus ENT2.

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Biological Activity

EOS301984 (EOS-984) is a potent, selective equilibrative nucleoside transporter 1 (ENT1) antagonist with IC50 of 339.6 nM (human ENT1), 150-fold selectivity for ENT1 versus ENT2.

EOS301984 (EOS-984) displays little to no inhibitory activity against ENT4 or CNT1, CNT2 or CNT3.

EOS301984 (EOS-984) binds to human and mouse ENT1 with Kd of 0.5 nM and 14.4 nM respectively.

EOS301984 (EOS-984) inhibited adenosine uptake into activated human T cells with sub-nanomolar potency and restored T cell proliferation both in the presence of adenosine and also dose-dependently in the presence of ATP acting as a source of adenosine.

EOS301984 (EOS-984) dose-dependently increased the levels of UMP, UDP, UTP and CTP in adenosine-treated T cells while also reducing adenosine-driven increases in carbamoyl aspartate, DHO and orotate.

EOS301984 (EOS-984) can restore T cell and tumor-infiltrating lymphocyte (TIL) expansion and effector function in high-adenosine environments.

EOS301984 (EOS-984) combined with anti-PD-1, can control tumor growth in a humanized mouse model of triple-negative breast cancer that is normally resistant to anti-PD-1 blockade.

Physicochemical Properties

M.Wt	629.75
Formula	C33H47N3O9
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(12R)-74,75-dimethoxy-6-oxo-8-oxa-5-aza-1(1,4)-diazepana-7(1,3)-benzenacyclotetradecaphane-12-yl 3,4,5-trimethoxybenzoate

References

1. Patent WO2021204896 A1.
2. Theodore J Sanders, et al. Nat Immunol. 2025 May 12. doi: 10.1038/s41590-025-02153-3.

EOS301984 (EOS984, EOS-984, EOS-301984)

Biological Activity

Physicochemical Properties

References

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