General description
一种具有口服活性的IDO1抑制剂，IC50：38nM，具有潜在的免疫调节和抗肿瘤活性。
NLG919 is an orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, NLG919 targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the essential amino acid tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, this agent increases tryptophan levels, restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, T-lymphocytes, and causes a reduction in tumor-associated regulatory T-cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells。
NLG919是一种吲哚胺2，3-二加氧酶1（IDO1）的口服抑制剂，具有潜在的免疫调节和抗肿瘤活性。 给药后，NLG919靶向并与IDO1结合，IDO1是负责将必需氨基酸色氨酸氧化成犬尿氨酸的细胞溶酶。 通过抑制IDO1并减少肿瘤细胞中的犬尿氨酸，该药物可提高色氨酸水平，恢复各种免疫细胞（包括树突状细胞（DC），自然杀伤性（NK）细胞，T淋巴细胞）的增殖和活化，并导致肿瘤减少 相关的调节性T细胞（Tregs）。 在许多癌症中被抑制的免疫系统激活可能诱导针对表达IDO1的肿瘤细胞的细胞毒性T淋巴细胞（CTL）反应。
Properties
| Iupac Name： | 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol |
| Inchi Code | 1S/C18H22N2O/c21-18(13-6-2-1-3-7-13)10-16-14-8-4-5-9-15(14)17-11-19-12-20(16)17/h4-5,8-9,11-13,16,18,21H,1-3,6-7,10H2 |
| Inchi Key | YTRRAUACYORZLX-UHFFFAOYSA-N |
安全信息
