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  • 产品名称： Pexidartinib
  • 产品货号： CS2115
  • 货期： 现货
  • 价格与订购： 300
  • 数量：
    库存： 100
  • 规格： 2mg 5mg
  • 产品信息
  • 如何订购
    产品描述
    Navoximod (NLG-​919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki/EC50: 7 nM/75 nM).
    体外活性
    Using IDO-expressing human monocyte-derived dendritic cells (DCs) in allogeneic mixed lymphocyte reaction (MLR) reactions, Navoximod potently blocks IDO-induced T cell suppression and restores robust T cell responses (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 (ED50: 120 nM) [1]. 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: 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 tumor cells although slightly less potent than Navoximod [3].
    产品描述
    Pexidartinib is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
    靶点活性
    CSF-1R    FLT3    Kit
    体外活性
    In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. [1]
    体内活性
    In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6 g−F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. [1] In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. [2] In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. [3] In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. [4]
    参考文献
    1. DeNardo DG, et al. Cancer Discov. 2011, 1(1), 54-67.
     
    2. Coniglio SJ, et al. Mol Med. 2012, 18, 519-527.
     
    3. Chitu V, et al. Blood. 2012, 120(15), 3126-3135.
     
    4. Sluijter M, et al. PLoS One. 2014, 9(8), e104230.
     
    5. Fan K, Li Y, Wang H, et al. Stress-Induced Metabolic Disorder in Peripheral CD4+ T Cells Leads to Anxiety-like Behavior[J]. Cell. 2019, 179(4): 864-879. e19.
    别名
    PLX-3397
    纯度
    99.66%
    分子量
    417.81
    分子式
    C20H15ClF3N5
    CAS No
    1029044-16-3
    存储
     for short term (days to weeks), or -20℃ for long term (months).
    溶解度
    DMSO: 77 mg/mL (184.3 mM)
                Ethanol: <1 mg/mL
               ( < 1 mg/ml refers to the product slightly soluble or insoluble )
    icon
    Note
    For research use only .
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