受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H15ClF3N5 |
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分子量 | 417.81 | CAS No. | 1029044-16-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 84 mg/mL (201.04 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3. |
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in vitro | 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] |
in vivo | In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−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] |
キナーゼアッセイ | Kinase assay | |
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PLX3397 is identified as a potent CSF-1R and c-KIT kinase inhibitor by using a Scaffold- and X-ray structure-based discovery approach. The IC50 data are from SelectScreen™ profiling service. | ||
細胞アッセイ | 細胞株 | Myelinating cultures |
濃度 | 1 uM | |
反応時間 | ||
実験の流れ | Myelinating cultures were treated with hemin or vehicle control in the absence or presence of PLX3397. |
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動物実験 | 動物モデル | MMTV-PyMT mice |
投薬量 | 40 mg/kg/day | |
投与方法 | p.o. |
Data from [Data independently produced by , , Nat Commun, 2017, 8:14293]
Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(20):6021-6030]
Data from [Data independently produced by , , Brain Behav Immun, 2018, 68:248-260]
The aging mouse CNS is protected by an autophagy-dependent microglia population promoted by IL-34 [ Nat Commun, 2024, 15(1):383] | PubMed: 38195627 |
Host-functionalization of macrin nanoparticles to enable drug loading and control tumor-associated macrophage phenotype [ Front Immunol, 2024, 15:1331480] | PubMed: 38545103 |
Microglia-endothelial cross-talk regulates diabetes-induced retinal vascular dysfunction through remodeling inflammatory microenvironment [ iScience, 2024, 27(3):109145] | PubMed: 38414848 |
Colony stimulating factor-1 (CSF-1) signalling is predictive of response to immune checkpoint inhibitors in advanced non-small cell lung cancer [ Lung Cancer, 2024, 188:107447] | PubMed: 38176297 |
Engineering an inhibitor-resistant human CSF1R variant for microglia replacement [ J Exp Med, 2023, 220(3)e20220857] | PubMed: 36584406 |
Polyoxazoline-Based Nanovaccine Synergizes with Tumor-Associated Macrophage Targeting and Anti-PD-1 Immunotherapy against Solid Tumors [ Adv Sci (Weinh), 2023, 10(25):e2300299] | PubMed: 37434063 |
The type-I interferon response potentiates seeded tau aggregation and exacerbates tau pathology [ Alzheimers Dement, 2023, 10.1002/alz.13493] | PubMed: 37849026 |
Repopulated retinal microglia promote Müller glia reprogramming and preserve visual function in retinal degenerative mice [ Theranostics, 2023, 13(5):1698-1715] | PubMed: 37056562 |
Meningeal macrophages inhibit chemokine signaling in pre-tumor cells to suppress mouse medulloblastoma initiation [ Dev Cell, 2023, 10.1038/s41418-023-01234-w] | PubMed: 37774709 |
ZIC2 induces pro-tumor macrophage polarization in nasopharyngeal carcinoma by activating the JUNB/MCSF axis [ Cell Death Dis, 2023, 14(7):455] | PubMed: 37479694 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。