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MedKoo Cat#: 206165 | Name: NLG919 (GDC-0919)
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

NLG919 (GDC-0919)
CAS#1402836-58-1

Theoretical Analysis

MedKoo Cat#: 206165

Name: NLG919 (GDC-0919)

CAS#: 1402836-58-1

Chemical Formula: C18H22N2O

Exact Mass: 282.1732

Molecular Weight: 282.38

Elemental Analysis: C, 76.56; H, 7.85; N, 9.92; O, 5.67

Price and Availability

Size Price Availability Quantity
10mg USD 110.00 Ready to ship
25mg USD 220.00 Ready to ship
50mg USD 400.00 Ready to ship
100mg USD 700.00 Ready to ship
250mg USD 1,250.00 Ready to ship
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Related CAS #
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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
InChi Key
YTRRAUACYORZLX-UHFFFAOYSA-N
InChi Code
InChI=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
SMILES Code
OC(C1CCCCC1)CC(C2=C3C=CC=C2)N4C3=CN=C4
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO (15 mg/ mL) and ethanol (14 mg/mL), not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
        
Biological target:
NLG-919 analogue is a potent IDO1 inhibitor with an IC50 of 38 nM.
In vitro activity:
In this study, a dual functional drug conjugate comprised of protoporphyrin IX and NLG919, a potent indoleamine-2,3-dioxygenase (IDO) inhibitor, is designed to combine photodynamic therapy and immune checkpoint blockade to achieve both primary tumor and distant metastases inhibition. Liposomal delivery is applied to improve the biocompatibility and tumor accumulation of the drug conjugate (PpIX-NLG@Lipo). The in vitro and in vivo experiments demonstrated that PpIX-NLG@Lipo possess strong ability of ROS generation to damage cancer cells directly through PDT. Meanwhile, PpIX-NLG@ Lipo can induce immunogenic cell death to elicit the host immune system. Furthermore, PpIX-NLG@Lipo interferes the activity of IDO, which can amplify PDT-induced immune responses, leading to an increasing amount of CD8+ T lymphocytes infiltrated into tumor site, finally achieve both primary and distant tumor inhibition. Theranostics. 2019; 9(19): 5542–5557.Published online 2019 Jul 29. doi: 10.7150/thno.35343 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6735384/
In vivo activity:
This study used 4T1 breast cancer cells to examine the anthracycline DOX-mediated immunogenic death of breast tumor cells by assessing the calreticulin exposure and adenosine triphosphate and high mobility group box 1 release. Using 4T1 tumor cell-engrafted mouse model, the study also detected the expression of indoleamine 2,3-dioxygenase (IDO) in tumor tissues after DOX treatment and further explored whether the specific small molecule IDO1 inhibitor NLG919 combined with DOX, can exhibit better therapeutic effects on breast cancer. Treatment with NLG919 enhanced kynurenine inhibition in a dose-dependent manner. IDO1 inhibition reversed CD8+ T cell suppression mediated by IDO-expressing 4T1 murine breast cancer cells. Compared to single agent therapy, combination of NLG919 with DOX demonstrated better therapeutic effects in 4T1 murine breast tumor model. IDO inhibition by NLG919 enhanced the therapeutic efficacy of DOX in breast cancer, achieving synergistic effect. J Breast Cancer. 2019 Apr 24;22(2):196-209. doi: 10.4048/jbc.2019.22.e23. eCollection 2019 Jun. https://pubmed.ncbi.nlm.nih.gov/31281723/
Solvent mg/mL mM comments
Solubility
DMSO 16.0 56.70
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 282.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1.Huang Z, Wei G, Zeng Z, Huang Y, Huang L, Shen Y, Sun X, Xu C, Zhao C. Enhanced cancer therapy through synergetic photodynamic/immune checkpoint blockade mediated by a liposomal conjugate comprised of porphyrin and IDO inhibitor. Theranostics. 2019 Jul 29;9(19):5542-5557. doi: 10.7150/thno.35343. PMID: 31534502; PMCID: PMC6735384. 2. Jiang X, Li X, Zheng S, Du G, Ma J, Zhang L, Wang H, Tian J. Comparison study of different indoleamine-2,3 dioxygenase inhibitors from the perspective of pharmacodynamic effects. Int J Immunopathol Pharmacol. 2020 Jan-Dec;34:2058738420950584. doi: 10.1177/2058738420950584. PMID: 32962460; PMCID: PMC7517983. 3. Gao J, Deng F, Jia W. Inhibition of Indoleamine 2,3-Dioxygenase Enhances the Therapeutic Efficacy of Immunogenic Chemotherapeutics in Breast Cancer. J Breast Cancer. 2019 Apr 24;22(2):196-209. doi: 10.4048/jbc.2019.22.e23. PMID: 31281723; PMCID: PMC6597411 4. Huang Z, Wei G, Zeng Z, Huang Y, Huang L, Shen Y, Sun X, Xu C, Zhao C. Enhanced cancer therapy through synergetic photodynamic/immune checkpoint blockade mediated by a liposomal conjugate comprised of porphyrin and IDO inhibitor. Theranostics. 2019 Jul 29;9(19):5542-5557. doi: 10.7150/thno.35343. PMID: 31534502; PMCID: PMC6735384.
In vitro protocol:
1.Huang Z, Wei G, Zeng Z, Huang Y, Huang L, Shen Y, Sun X, Xu C, Zhao C. Enhanced cancer therapy through synergetic photodynamic/immune checkpoint blockade mediated by a liposomal conjugate comprised of porphyrin and IDO inhibitor. Theranostics. 2019 Jul 29;9(19):5542-5557. doi: 10.7150/thno.35343. PMID: 31534502; PMCID: PMC6735384. 2. Jiang X, Li X, Zheng S, Du G, Ma J, Zhang L, Wang H, Tian J. Comparison study of different indoleamine-2,3 dioxygenase inhibitors from the perspective of pharmacodynamic effects. Int J Immunopathol Pharmacol. 2020 Jan-Dec;34:2058738420950584. doi: 10.1177/2058738420950584. PMID: 32962460; PMCID: PMC7517983.
In vivo protocol:
1.Gao J, Deng F, Jia W. Inhibition of Indoleamine 2,3-Dioxygenase Enhances the Therapeutic Efficacy of Immunogenic Chemotherapeutics in Breast Cancer. J Breast Cancer. 2019 Apr 24;22(2):196-209. doi: 10.4048/jbc.2019.22.e23. PMID: 31281723; PMCID: PMC6597411. 2. Huang Z, Wei G, Zeng Z, Huang Y, Huang L, Shen Y, Sun X, Xu C, Zhao C. Enhanced cancer therapy through synergetic photodynamic/immune checkpoint blockade mediated by a liposomal conjugate comprised of porphyrin and IDO inhibitor. Theranostics. 2019 Jul 29;9(19):5542-5557. doi: 10.7150/thno.35343. PMID: 31534502; PMCID: PMC6735384.
1: Vacchelli E, Aranda F, Eggermont A, Sautès-Fridman C, Tartour E, Kennedy EP, Platten M, Zitvogel L, Kroemer G, Galluzzi L. Trial watch: IDO inhibitors in cancer therapy. Oncoimmunology. 2014 Dec 15;3(10):e957994. Review. PubMed PMID: 25941578; PubMed Central PMCID: PMC4292223. 2: 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. PubMed PMID: 25054064; PubMed Central PMCID: PMC4105871. 3: Peng YH, Ueng SH, Tseng CT, Hung MS, Song JS, Wu JS, Liao FY, Fan YS, Wu MH, Hsiao WC, Hsueh CC, Lin SY, Cheng CY, Tu CH, Lee LC, Cheng MF, Shia KS, Shih C, Wu SY. Important Hydrogen Bond Networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Design Revealed by Crystal Structures of Imidazoleisoindole Derivatives with IDO1. J Med Chem. 2016 Jan 14;59(1):282-93. doi: 10.1021/acs.jmedchem.5b01390. PubMed PMID: 26642377. 4: Chen Y, Xia R, Huang Y, Zhao W, Li J, Zhang X, Wang P, Venkataramanan R, Fan J, Xie W, Ma X, Lu B, Li S. An immunostimulatory dual-functional nanocarrier that improves cancer immunochemotherapy. Nat Commun. 2016 Nov 7;7:13443. doi: 10.1038/ncomms13443. PubMed PMID: 27819653; PubMed Central PMCID: PMC5103075.

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