1402836-58-1 Usage
Description
(±)-NLG-919 is an indoleamine 2,3-dioxygenase (IDO) pathway inhibitor (Ki = 7 nM; EC50 = 75 nM). (±)-NLG-919 inhibits IDO-induced T cell suppression and restores T cell response during allogenic mixed lymphocyte reactions in vitro (ED50s = 80 and 120 nM, respectively). In vivo, (±)-NLG-919 induces a 95% reduction in tumor volume when administered in conjunction with a pmel-1 T cell vaccine. Formulations containing (±)-NLG-919 are under investigation in clinical trials for treatment of glioblastoma, melanoma, pancreatic, and breast cancers.
Uses
NLG919 is a potent indoleamine-2,3-dioxygenase (IDO) pathway inhibitor and is suitable for the treatment of immunosuppression associated with cancer.
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.
