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

Chemical Structure : EOS301984

CAS No.: 2724937-55-5

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

货号: 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.

规格	价格	库存
1 mg	￥3780	In stock
2 mg	￥5780	In stock
5 mg		Get quote
10 mg		Get quote
25 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	629.75
分子式	C33H47N3O9
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	(12R)-74,75-dimethoxy-6-oxo-8-oxa-5-aza-1(1,4)-diazepana-7(1,3)-benzenacyclotetradecaphane-12-yl 3,4,5-trimethoxybenzoate

参考文献

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)

生物&药学活性

物理化学性质&存储条件

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

生物&药学活性

物理化学性质&存储条件

参考文献

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