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Information Navoximod Navoximod (GDC-0919, NLG-919) is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) pathway with Ki of 7 nM and EC50 of 75 nM. Targets IDO (Cell-free assay); IDO (Cell-free assay) 7 nM(Ki); 75 nM(EC50) In vitro 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) with ED50 of 120 nM.\xa0NLG919 increases the cytotoxic activity of paclitaxel toward B16-F10 cells in the presence of pretreatment with interferon (IFN)-γ in vitro. 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.Immune competent mice are injected orthotopically with genetically engineered murine glioma cells and treated with GDC-0919 alone or combined with RT. GDC-0919 demonstrates potent inhibition of this node and effectively crosses the blood brain barrier. Although GDC-0919 as a single agent does not demonstrate anti-tumor activity, it has a strong potential for enhancing RT response in glioblastoma, which is further augmented with a hypofractionated regimen. Cell Research(from reference) Cell lines:the murine melanoma cell line B16-F10 Concentrations:100\u2009nM Incubation Time:12\u2009h, 24\u2009h, 48\u2009h, 72\u2009h
中文名称
纳沃西莫德
英文名称
Navoximod
中文别名
-
英文别名
NLG-919 | NLG-919 Navoximod | US10233190, Example 1484 | F85292 | (1R,4r)-4-((R)-2-((S)-6-fluoro-5H-imidazo[5,1- a]isoindol-5-yl)-1-hydroxyethyl)cyclohexanol | Navoximod | Navoximod;GDC-0919;IDO-IN-7;NLG-1488 | NAVOXIMOD [INN] | NLG-?919 | UNII-926SHL95NC
CAS号
1402837-78-8
分子式
C18H21FN2O2
分子量
316.37 g/mol
精确质量
10mM in DMSO
PSA
58.300 Ų
Logp
2.224
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纳沃西莫德 1ml

IDO/TDO 抑制剂

品牌:阿拉丁
货号:N421507-1ml
级别: 10mM in DMSO
货期:30天
已售 275 件
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