Structure of IDO-IN-7
CAS No.: 1402836-58-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H332-H335 |
Precautionary Statements: | P261-P280-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
CT26 colorectal tumor cells | 1 μM | 24 hours | Evaluate cytotoxicity of HCNSP and HCNCP, results showed cell viability over 80% | PMC7175291 |
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. | PMC9214055 |
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). | PMC9214055 |
CTLL-2 cells | 100 μM | 24 hours | Increased IL-2 secretion by approximately 80% | PMC11735626 |
MDA-MB-231 cells | 100 μM | 24 hours | Induced ICD, reduced proportion of Tregs among CD4+ T cells | PMC11735626 |
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% | PMC11735626 |
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. | PMC11132052 |
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. | PMC8958467 |
CT26 colorectal tumor cells | 1 μM | 4 hours | Detect intracellular ROS generation, results showed significant increase in ROS upon laser irradiation | PMC7175291 |
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. | PMC8958467 |
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. | PMC5103075 |
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 | PMC10250924 |
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. | PMC5520195 |
PANC02 cells | 750 ng/mL | 5 hours | Evaluate the cellular uptake capability of PGEM carrier | PMC7183357 |
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. | PMC10724419 |
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. | PMC11132052 |
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. | PMC6662090 |
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. | PMC8466812 |
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. | PMC11097415 |
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. | PMC8958467 |
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 | PMC8201842 |
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. | PMC11786678 |
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 | PMC7183357 |
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. | PMC11132052 |
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. | PMC10724419 |
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. | PMC5103075 |
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 | PMC10250924 |
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. | PMC11401275 |
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. | PMC11378416 |
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 | PMC7175291 |
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 | PMC11735626 |
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. | PMC4105871 |
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 | PMC6735384 |
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 | PMC10213972 |
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 | PMC8187673 |
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. | PMC9214055 |
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 | PMC11223770 |
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 << |
Tags: IDO-IN-7 | NLG-919 analogue | GDC-0919 analogue | Indoleamine 2 |3-Dioxygenase (IDO) | IDO1 inhibitor | tryptophan metabolism | immune escape | cancer immunotherapy | indoleamine 2 |3-dioxygenase 1 | 1402836-58-1
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