| CAS NO: | 1402836-58-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 282.38 |
|---|---|
| Formula | C18H22N2O |
| CAS No. | 1402836-58-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 15 mg/mL warmed (53.1 mM) |
| Water: <1 mg/mL | |
| Ethanol: 30 mg/mL (106.2 mM) | |
| SMILES Code | OC(C1CCCCC1)CC(C2=C3C=CC=C2)N4C3=CN=C4 |
| Synonyms | IDO-IN 7; IDO IN 7; RG6078 analog; GDC-0919; IDO IN-7; GDC0919 analog; GDC 0919; NLG919; NLG 919 analog; NLG-919; RG-6078; RG 6078. |
| In Vitro | In vitro activity: NLG919 potently blocks IDO-induced T-cell suppression and restored robust T-cell responses with ED50 of 80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED50 of 120 NM. Kinase Assay: IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM. Cell Assay: NLG919 potently blockes IDO-induced T cell suppression and restores robust T cell responses with an EC50=90 nM. NLG919 also abrogates IDO-induced suppression of antigen-specific T cells (OT-I or pmel-1) in vitro, (ED50=130 nM ) using mouse IDO+ pDCs from tumor-draining lymph nodes. |
|---|---|
| In Vivo | In mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ~ 50%. In mice bearing B16F10 tumors, NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA. |
| Animal model | Mice bearing large established B16F10 tumor |
| Formulation & Dosage | Dissolved in water at 3 mg/mL; 6 mg/day injected via IP, or administered subcutaneously at 1 mg/dose twice a day via injection plus 360 μg/day via an SC osmotic pump. |
| References | J Immunother Cancer. 2014 Jul 7;2:21; AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 491. |
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