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Chemical Structure| 1402836-58-1 Chemical Structure| 1402836-58-1

Structure of IDO-IN-7
CAS No.: 1402836-58-1

Chemical Structure| 1402836-58-1

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NLG919 is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM in cell-free assays.

Synonyms: NLG919; GDC-0919 analogue; GDC-0919

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Product Details of IDO-IN-7

CAS No. :1402836-58-1
Formula : C18H22N2O
M.W : 282.38
SMILES Code : OC(C1CCCCC1)CC(C2=C3C=CC=C2)N4C3=CN=C4
Synonyms :
NLG919; GDC-0919 analogue; GDC-0919
MDL No. :MFCD26142661
InChI Key :YTRRAUACYORZLX-UHFFFAOYSA-N
Pubchem ID :66558287

Safety of IDO-IN-7

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CTLL-2 cells 100  µM 24 hours Increased IL-2 secretion by approximately 80% Nat Commun. 2025 Jan 15;16(1):687.
PANC02 cells 750 ng/mL 5 hours Evaluate the cellular uptake capability of PGEM carrier Acta Biomater. 2020 Apr 1;106:289-300.
CT26 colorectal tumor cells 1 µM 24 hours Evaluate cytotoxicity of HCNSP and HCNCP, results showed cell viability over 80% Adv Sci (Weinh). 2020 Feb 25;7(8):1903332.
CT26 murine colorectal tumor cells 4.0 μg/mL 24 hours Confirmed the inhibitory effect of NJ NPs on IFN-γ-induced IDO-1 activity, demonstrating a significant reduction in the Kyn/Trp ratio. Acta Pharm Sin B. 2022 Jun;12(6):2695-2709.
4T1 murine breast tumor cells 10 µM 24 hours Evaluated the photoactivity and ROS generation of PHPNJ NPs, showing significantly increased ROS production under acidic conditions (pH 6.5). Acta Pharm Sin B. 2022 Jun;12(6):2695-2709.
MDA-MB-231 cells 100  µM 24 hours Induced ICD, reduced proportion of Tregs among CD4+ T cells Nat Commun. 2025 Jan 15;16(1):687.
4T1 cells 100  µM 24 hours Induced immunogenic cell death (ICD), increased ATP release by 5.2-fold, HMGB1 release by 2.4-fold, and CRT surface exposure by ~30% Nat Commun. 2025 Jan 15;16(1):687.
B16 tumor cells 50 µM 24 hours Evaluate the cytotoxicity of NCSNPs on B16 tumor cells and their effect on inducing pyroptosis. Results showed that NCSNPs significantly induced pyroptosis and inhibited tumor cell proliferation. Adv Sci (Weinh). 2024 May;11(20):e2305382.
Lymphocyte-HeLa cells co-culture system 20 µM 3 days Assess whether BN@HM-OVA can reverse the inhibition of T cell proliferation caused by IDO. Results showed that BN@HM-OVA nanovaccine effectively stimulated T cell proliferation. Bioact Mater. 2022 Mar 11;16:107-119.
CT26 colorectal tumor cells 1 µM 4 hours Detect intracellular ROS generation, results showed significant increase in ROS upon laser irradiation Adv Sci (Weinh). 2020 Feb 25;7(8):1903332.
HeLa cells 0–30 µM 48 hours Evaluate the inhibitory effect of NLG-919 on IDO enzyme activity. Results showed that BN@HM-OVA nanovaccine inhibited IDO activity in a concentration-dependent manner. Bioact Mater. 2022 Mar 11;16:107-119.
HeLa cells 50 nM–20 µM 48 hours To evaluate the inhibitory effect of PEG2k-Fmoc-NLG on IDO activity, results showed that PEG2k-Fmoc-NLG(L) and PEG2k-Fmoc-NLG(S) could inhibit IDO activity, but were less active than free NLG919. Nat Commun. 2016 Nov 7;7:13443.
HOS cells 10 µM 48 hours Evaluate the anti-tumor activity of NP-Pt-IDOi on HOS cells, results showed NP-Pt-IDOi had the highest cytotoxicity and promoted apoptosis Mater Today Bio. 2023 May 24;20:100675.
HeLa cells 50 nM –20 µM 48 hours To test the IDO inhibitory activity of PSSN10, results showed PSSN10 blocked IDO function in a concentration-dependent manner. Acta Pharmacol Sin. 2017 Jun;38(6):823-834.
Panc02 cells 25 μg/mL 6 hours To evaluate intracellular H2S release and ROS production. Results showed that H2S levels and ROS signal intensity were significantly increased in SPNDNH group. Adv Sci (Weinh). 2023 Dec;10(35):e2305150.
Human umbilical vein endothelial cells (HUVECs) 10–60 µM Evaluate the toxicity of NCSNPs on normal cells. Results showed that NCSNPs had minimal impact on the viability of HUVECs, indicating their safety for normal cells. Adv Sci (Weinh). 2024 May;11(20):e2305382.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Female Balb/C mice 4T1 mammary tumor model Intraperitoneal injection 10 mg/kg Once a day, started on day 12 and stopped on day 26 of experiments The combination of NLG919 with PLG-CA4 and PI3Kγ inhibitor significantly suppressed the growth of breast cancer and improved the tumor suppression rate. Adv Sci (Weinh). 2019 Apr 18;6(12):1900327
C57BL/6 mice PANC02 pancreatic cancer model Intravenous injection 10 mg/kg (NLG dosage) Two injections at an interval of 2 days, followed by laser irradiation at 24 h after the second injection, and then three more injections at an interval of four days. Evaluate the anti-tumor effect of N/PGEM/dp-16 NPs under laser irradiation. Results showed that N/PGEM/dp-16 NPs combined with laser irradiation significantly inhibited tumor growth, with negligible toxicity to liver and kidney. Biomaterials. 2021 Feb;269:120629
C57 mice Panc02 tumor-bearing model Tail vein injection 16 mg/kg Administered on the 1st, 4th, and 7th days NLG919 improved the 5-FU-induced tumor immunosuppressive microenvironment by inhibiting the Kyn-AHR axis, enhancing the effect of chemoimmunotherapy. J Nanobiotechnology. 2024 May 16;22(1):257
C57BL/6 mice E.G7-OVA tumor model Intratumoral injection 2 mg/kg per injection Every 4 days for 3 times Evaluate the antitumor efficacy of BN@HM-OVA nanovaccine in the E.G7-OVA tumor model. Results showed that BN@HM-OVA significantly inhibited tumor growth and prolonged survival in mice. Bioact Mater. 2022 Mar 11;16:107-119.
C57BL/6 mice B16F10 tumor model Intratumoral injection 2.5 mg/kg On Day 0, 3, and 6, total of three doses Evaluate the antitumor efficacy of PPF NPs combined with irradiation, showing significant tumor suppression with complete tumor eradication in 30% of mice and successful rejection of a second tumor inoculation J Nanobiotechnology. 2021 Jun 14;19(1):182
C57BL/6JGpt mice KPC pancreatic cancer mouse model Intravenous injection 2.8 mg/kg Every 3 days until tumor volume reached 1500 mm³ Evaluate the antitumor efficacy of DNMCs in the KPC pancreatic cancer mouse model, results showed that DNMCs significantly inhibited tumor growth without substantial weight loss. Mater Today Bio. 2025 Jan 13;31:101487
C57BL/6 mice PANC02 pancreatic tumor model Intravenous injection 20 mg/kg Every five days for a total of 6 times Evaluate the anti-tumor effect of PGEM carrier co-loaded with PTX and NLG919 Acta Biomater. 2020 Apr 1;106:289-300.
Mice B16 tumor model Intravenous injection 20 mg/kg NLG, 31.2 mg/kg SNAP Every 2 days, duration not specified Evaluate the antitumor efficacy of NCSNPs in the B16 tumor model. Results showed that NCSNPs significantly inhibited tumor growth and promoted immune responses. Adv Sci (Weinh). 2024 May;11(20):e2305382.
C57BL/6 mice Orthotopic pancreatic cancer model Intravenous injection 200 μg/mL Injection on day 0, 2, and 4; US irradiation on day 1, 3, and 5, repeated three times To evaluate antitumor and anti-metastasis effects. Results showed that tumor growth was almost completely inhibited and metastasis was significantly restricted in SPNDNH+US group. Adv Sci (Weinh). 2023 Dec;10(35):e2305150.
BALB/c mice 4T1.2 breast cancer model Intravenous injection 25 mg/kg Once every 3 days for 5 times To evaluate the in vivo antitumor activity of PEG2k-Fmoc-NLG(L), results showed that PEG2k-Fmoc-NLG(L) significantly inhibited tumor growth and enhanced T-cell immune responses. Nat Commun. 2016 Nov 7;7:13443.
Mice Orthotopic osteosarcoma model Intravenous injection 3.5 mg/kg Pt, 25 mg/kg NLG919 Three injections, lasting 20 days Evaluate the anti-tumor activity of NP-Pt-IDOi in the orthotopic osteosarcoma mouse model, results showed NP-Pt-IDOi significantly inhibited tumor growth, activated the STING pathway, and remodeled the tumor microenvironment Mater Today Bio. 2023 May 24;20:100675.
BALB/c mice 4T1 breast cancer model Tail vein injection 4 mg/kg (Ce6 concentration) and 2.4 mg/kg (NLG919 concentration) Every 3.5 days for a total of 4 cycles Evaluate the therapeutic effect of NLG919@CF nanoparticles combined with anti-PD-1 antibody on breast cancer bone metastasis. Results showed that tumor volume and bone destruction were significantly reduced in the NLG919@CF + L + anti-PD-1 group. J Nanobiotechnology. 2024 Sep 14;22(1):566
BALB/c mice CT26 tumor-bearing mouse model Intravenous injection 5 mg/kg Every 5 days, total 2 times Evaluate the antitumor effect of RIMNA in vivo, results showed that RIMNA combined with laser irradiation significantly inhibited the growth of primary and distant tumors and prolonged the survival time of mice. J Nanobiotechnology. 2024 Sep 5;22(1):542
Balb/c mice CT26 colorectal tumor model Intravenous injection 5.0 mg/kg PPa and 2.6 mg/kg NLG919 Every 3 days for 3 times Evaluate antitumor efficacy of HCNSP, results showed HCNSP+Laser significantly inhibited tumor growth and prolonged survival Adv Sci (Weinh). 2020 Feb 25;7(8):1903332.
Female BALB/c mice 4T1 tumor model In situ injection 5.7 mg/kg Abe and 31.8 mg/kg NLG919 Single dose, sustained for 7 days Reduced tumor recurrence and pulmonary metastasis, prolonged survival, inhibited IDO-1 activity, increased CTL infiltration and activity Nat Commun. 2025 Jan 15;16(1):687.
Mice Orthotopic glioblastoma model Oral 6 mg/mL Continuously starting at day 7 IDO blockade synergized with chemo-radiation therapy to significantly prolong survival in mice bearing intracranial glioblastoma and triggered widespread complement deposition within tumors. J Immunother Cancer. 2014 Jul 7;2:21
BALB/c female mice Bilateral 4T1 tumor model Intravenous injection 6 μmol/kg Every two days for a total of three injections Evaluate the inhibitory effect of PpIX-NLG@Lipo on primary and distant tumors in vivo Theranostics. 2019 Jul 29;9(19):5542-5557
BALB/c mice 4T1 breast cancer model Tail vein injection 6.5 mg/kg Every 3 days, 3 times in total To evaluate the anti-tumor effect of NLG919@Lip-pep1, results showed a tumor growth inhibition rate of 73% and significantly reduced lung metastatic nodules Acta Pharm Sin B. 2023 May;13(5):2176-2187
Balb/c mice Subcutaneous CT26 colon tumor model and orthotopic 4T1 breast tumor model Intravenous injection DOX 5 mg/kg, aNLG919 25 mg/kg Injections at day 0, 3, and 6 To evaluate the antitumor efficacy of DNCaNPs, showing significant tumor growth suppression and extended survival Nanomicro Lett. 2020 Nov 22;13(1):29.
BALB/c mice 4T1 breast tumor model and CT26 colorectal tumor model Intravenous injection NLG919 10 mg/kg, JQ1 15 mg/kg Every 3 days for 5 doses Assessed the antitumor efficacy and immunomodulatory effects of PHPNJ NPs, showing significant tumor growth inhibition, prolonged survival, enhanced CD8? T cell infiltration, and reduced Tregs. Acta Pharm Sin B. 2022 Jun;12(6):2695-2709.
BALB/c mice 4T1 breast cancer model Intravenous injection NLG919 5 mg/kg, MSA-2 2.4 mg/kg Every 2 days for a total of 3 times Evaluated antitumor efficacy of MN NPs, showing significant tumor growth inhibition and immune activation Biomater Res. 2024 Jul 4;28:0048

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02048709 Solid Tumor PHASE1 COMPLETED 2025-02-16 Georgia Regents University, Au... More >>gusta, Georgia, 30912, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.71mL

3.54mL

1.77mL

35.41mL

7.08mL

3.54mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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