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Navoximod

CAS No. : 1402837-78-8

MCE 站：Navoximod

产品活性：Navoximod (GDC-0919; NLG-​919) 是一种有效的 IDO (indoleamine-(2,3)-dioxygenase) 抑制剂，K_i/EC₅₀ 分别为 7 nM/75 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Indoleamine 2,3-Dioxygenase (IDO)

In Vitro: Using IDO-expressing human monocyte-derived dendritic cells (DCs) in allogeneic mixed lymphocyte reaction (MLR) reactions, Navoximod (NLG919) potently blocks IDO-induced T cell suppression ａnd restores robust T cell responses with an ED₅₀=80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, Navoximod abrogates IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED₅₀=120 nM. Navoximod inhibits the IDO activity in a concentration-dependent manner with an EC₅₀ of 0.95 μM. PEG2k-Fmoc-NLG(L) is less active (EC₅₀ of 3.4 μM) in inhibiting IDO compared with free Navoximod while PEG2k-Fmoc-NLG(S) is least active (EC₅₀>10 μM). Coculture of IDO+tumor cells with splenocytes isolated from BALB/c mice leads to significant inhibition of T-cell proliferation. This inhibition is significantly attenuated when the mixed cells are treated with Navoximod. PEG2k-Fmoc-NLG(L) is also active in reversing the inhibitory effect of tumour cells although slightly less potent than Navoximod .

In Vivo: VNavoximod (NLG919) is orally bioavailable (F>70%); ａnd has a favorable pharmacokinetic ａnd toxicity profile. In mice, a single oral administration of Navoximod reduces the concentration of plasma ａnd tissue Kyn by ~50%. In vivo, in mice bearing large established B16F10 tumors, administration of Navoximod markedly enhances the anti-tumor responses of naïve, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA. In this stringent established-tumor model, Navoximod plus pmel-1/vaccine produce a dramatic collapse of tumor size within 4 days of vaccination (~95% reduction in tumor volume compare to control animals receiving pmel-1/vaccine alone without Navoximod). When combined with NSC 362856 (TMZ)+radiation therapy (RT), both Navoximod ａnd D-1MT (Indoximod) enhance survival relative to mice treated with TMZ+RT alone.

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