Name: NLG919 (GDC-0919)
CAS#: 1402836-58-1
Chemical Formula: C18H22N2O
Exact Mass: 282.17321
Molecular Weight: 282.38
Elemental Analysis: C, 76.56; H, 7.85; N, 9.92; O, 5.67
EOS Med Chem produce NLG919 (GDC-0919) 1402836-58-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
NLG919 (GDC-0919) 1402836-58-1 Intermediates, EOS Med Chem have 8; NLG919 (GDC-0919) 1402836-58-1 Impurity we have 10, all from GMP, FDA plant.
Now NLG919 (GDC-0919) 1402836-58-1 DMF document is preparing.
Until 2016, Aug, NLG919 (GDC-0919) 1402836-58-1 more than produced 25kg API, 120kg Intermediates
NLG-919 API and intermediates 96797-15-8 ≥98.0% 4-Iodo-1-tritylimidazole
NLG-920 API and intermediates 40138-16-7 ≥98.0% 2-Formylbenzeneboronic acid
NLG-921 API and intermediates 1402838-08-7 ≥98.0% 2-(1-trityl-1H-imidazol-4-yl)benzaldehyde
Synonym: GDC0919; GDC-0919; GDC 0919; NLG919; NLG 919; NLG-919; RG6078; RG-6078; RG 6078.
IUPAC/Chemical Name: 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol
SMILES Code: OC(C1CCCCC1)CC(C2=C3C=CC=C2)N4C3=CN=C4
Description: GDC-0919, also known as NLG919 and RG6078, 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.
1: Li M, Bolduc AR, Hoda MN, Gamble DN, Dolisca SB, Bolduc AK, Hoang K, Ashley C, McCall D, Rojiani AM, Maria BL, Rixe O, MacDonald TJ, Heeger PS, Mellor AL, Munn DH, Johnson TS. The indoleamine 2,3-dioxygenase pathway controls complement-dependent enhancement of chemo-radiation therapy against murine glioblastoma. J Immunother Cancer. 2014 Jul 7;2:21. doi: 10.1186/2051-1426-2-21. eCollection 2014. PubMed PMID: 25054064; PubMed Central PMCID: PMC4105871.
