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- 產(chǎn)品名稱： Pexidartinib
- 產(chǎn)品貨號： CS2115
- 貨期： 現(xiàn)貨
- 價格與訂購： 300
- 數(shù)量：
庫存： 100
- 規(guī)格： 2mg 5mg
- 產(chǎn)品信息
- 如何訂購
產(chǎn)品描述
Navoximod (NLG-?919, GDC-0919) is a potent indoleamine-(2,3)-dioxygenase (IDO) pathway inhibitor (Ki/EC50: 7 nM/75 nM).
體外活性
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].
產(chǎn)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.
靶點活性
CSF-1R FLT3 Kit
體外活性
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]
體內(nèi)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]
參考文獻
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.
別名
PLX-3397
純度
99.66%
分子量
417.81
分子式
C20H15ClF3N5
CAS No
1029044-16-3
存儲
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 )
Note
For research use only .
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