IDO-IN-2 CAS NO.914471-09-3

长沙雁飞生物科技有限公司位于国家生物产业基地——长沙市生物医药园,是一家致力于天然药物活性成分现代化、产业化研究,集开发、生产、销售高标准高质量高科技产品为一体的高新科技企业。 公司下设研发、生产、销售等多个部门。公司研发中心拥有多台高效液相色谱、紫外分析仪等先进检测实验仪器,配备人员均为本科及以上学历,对工艺研究、质量保证、质量检测三项职能进行了明细分工,以此对生产过程进行有效全面的质量控制,对最终产品进行全面检测,以确保产品品质。公司在高速发展的同时,坚持自主研发与合作研发相结合,与湖南、广东、上海等地多家高校和科研机构长期合作,为高纯度活性单体和标准化提取物工业化生产提供强有力的保障。

IDO-IN-2 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.
IC50 Value: 10 nM [1]
Target: IDO1
in vitro: In cellular assays,IDO-IN-2 selectively inhibits human IDO1 with IC(50) values of approximately 10nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO) [1]. In coculture systems of human allogeneic lymphocytes with dendritic cells (DCs) or tumor cells,IDO-IN-2 inhibition of IDO1 promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. IDO1 induction triggers DC apoptosis, whereas IDO-IN-2 reverses this and increases the number of CD86 (high) DCs, potentially representing a novel mechanism by which IDO1 inhibition activates T cells [1].
in vivo: Consistent with its effects in vitro, administration of IDO-IN-2 to tumor-bearing mice significantly inhibits tumor growth in a lymphocyte-dependent manner [1]. A single dose of IDO-IN-2 or IDO-IN-2 results in efficient and durable suppression of Ido1 activity in the plasma of treated mice and dogs, the former to levels seen in Ido1-deficient mice [2].
Clinical trial: A Phase 2 Study of the IDO Inhibitor IDO-IN-2 Versus Tamoxifen for Subjects With Biochemical-recurrent-only EOC, PPC or FTC Following Complete Remission With First-line Chemotherapy.