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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Indoleamine 2,3-Dioxygenase (IDO)-LY-3381916
LY-3381916

Chemical Structure : LY-3381916

CAS No.: 2166616-75-5

LY-3381916 (LY3381916)

货号: PC-73168Not For Human Use, Lab Use Only.

LY-3381916 is a potent, selective and brain-penetrant Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with IC50 of 7 nM.

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10 mg ¥1280 In stock
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50 mg ¥3680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LY-3381916 is a potent, selective and brain-penetrant Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with IC50 of 7 nM.
LY-3381916 displays no significant inhibitory activity against TDO2 (IC50>20 uM), shows no confounding agonism of AHR up to 100 uM.
LY3381916 occupies the heme-binding pocket of IDO1, binds to newly synthesized apo-IDO1 lacking heme, but does not inhibit mature heme-bound IDO1.
LY-3381916 exhibits substantial inhibition of IDO1 in tumors requires the turn-over of mature heme-bound IDO1.
LY-3381916 enhances anti-PD-L1 antibody (LY3300054) activity in pre-clinical tumor model.

物理化学性质&存储条件

分子量 396.45
分子式 C23H25FN2O3
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

(R)-4-Fluoro-N-(1-(1-(tetrahydro-2H-pyran-4-carbonyl)indolin-5-yl)ethyl)benzamide

参考文献

1. Frank C. Dorsey, et al. Cancer Res (2018) 78 (13_Supplement): 5245.

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