1402836-58-1 Usage
Description
NLG919, also known as (±)-NLG-919, is a potent indoleamine 2,3-dioxygenase (IDO) pathway inhibitor with significant potential in the treatment of immunosuppression associated with cancer. It effectively inhibits IDO-induced T cell suppression and restores T cell response, making it a promising candidate for various cancer therapies.
Uses
Used in Oncology:
NLG919 is used as an immunotherapy agent for the treatment of immunosuppression associated with cancer. It works by inhibiting the IDO pathway, which is often upregulated in cancer cells to suppress the immune system and promote tumor growth. By targeting this pathway, NLG919 can help restore the immune system's ability to recognize and attack cancer cells.
Used in Clinical Trials:
NLG919 is currently under investigation in clinical trials for the treatment of various types of cancer, including glioblastoma, melanoma, pancreatic, and breast cancers. These trials aim to evaluate the safety, efficacy, and optimal dosing regimens for NLG919 in combination with other cancer treatments, such as T cell vaccines.
Used in Drug Development:
As a potent IDO pathway inhibitor, NLG919 serves as a valuable compound in the development of new cancer therapies. Researchers and pharmaceutical companies can use NLG919 as a starting point for designing and synthesizing novel inhibitors targeting the IDO pathway, potentially leading to the discovery of more effective and selective cancer treatments.
Used in Combination Therapies:
NLG919 has demonstrated the potential to be used in combination with other cancer treatments, such as T cell vaccines. This approach can enhance the overall efficacy of cancer therapy by combining the immunostimulatory effects of NLG919 with the targeted action of vaccines, leading to a more comprehensive attack on cancer cells.
References
1) Mautino?et al.?(2013),?NLG919, a novel indolamine-2,3-dioxygenase (IDO)-pathway inhibitor drug candidate for cancer therapy;?Cancer Res.?73?issue 8 supplement?491
2) Li?et al.?(2014),?The indolamine 2,3-dioxygenase pathway controls complement-dependent enhancement of chemo-radiation therapy against murine glioblastoma;?J. Immunother. Cancer?2?21
3) Meng?et al.?(2017),?Combinatorial antitumor effects of indoleamine 2,3-dioxygenase inhibitor NLG919 and paclitaxel in a murine B16-F10 melanoma model;?Int. J. Immunopathol. Pharmacol.?30?215
Check Digit Verification of cas no
The CAS Registry Mumber 1402836-58-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,0,2,8,3 and 6 respectively; the second part has 2 digits, 5 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 1402836-58:
(9*1)+(8*4)+(7*0)+(6*2)+(5*8)+(4*3)+(3*6)+(2*5)+(1*8)=141
141 % 10 = 1
So 1402836-58-1 is a valid CAS Registry Number.
1402836-58-1Relevant articles and documents
Chiral resolution, absolute configuration determination, and stereo-activity relationship study of IDO1 inhibitor NLG919
Liu, Wen-Qiang,Lai, Fang-Fang,Zhang, Jie,Sheng, Li,Li, Yan,Li, Li,Chen, Xiao-Guang
, p. 3045 - 3051 (2018/05/16)
NLG919 (1) with two chiral carbon atoms on its chemical structure is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. We developed an effective way to prepare all stereoisomers of 1, the key step being the chiral resolution of racemic intermediate 2. The optimal resolution solvent system was identified as dichloromethane and n-pentane or petroleum ether. Using (?)-di-p-toluoyl-D-tartaric acid as resolution reagent, optical pure (R)-2 (e.e. > 99%, yield = 70%) was obtained. The mechanism of chiral resolution was clarified through single-crystal X-ray diffraction of the diastereomeric salt. The absolute configurations of four stereoisomers of 1 were established through electronic circular dichroism spectra, quantum chemical calculation and transition metal method. Their IDO1 inhibitory activity was assessed by pharmacological experiments in vitro and in mouse, demonstrating that S configuration of C5 played an important role on the inhibition of IDO1, while the stereochemistry on C2′ exerted little effect on the IDO1 inhibitory activity in mouse.
COMPOUNDS FOR THE INHIBITION OF INDOLEAMINE-2,3-DIOXYGENASE
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, (2016/04/09)
The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.
