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CAS No. : 2222138-31-8
MCE 国际站:Sotuletinib hydrochloride
产品活性:Sotuletinib (BLZ945) 是一种有效,选择性和脑渗透性的 CSF-1R (c-Fms) 抑制剂,IC50 为 1 nM,选择性是其他受体酪氨酸激酶同系物的 1000 倍。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:c-Fms
In Vitro: Sotuletinib hydrochloride inhibits CSF-1-dependent proliferation (EC50=67 nM) in bone marrow-derived macrophages (BMDMs), and decreases CSF-1R phosphorylation, similar to CSF-1R antibody blockade. Sotuletinib hydrochloride also reduces viability of CRL-2467 microglia, Ink4a/Arf?/? BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, Sotuletinib hydrochloride treatment in culture does not affect proliferation of any PDG-derived tumor cell lines (all Csf-1r-negative), or U-87 MG human glioma cells, and PDG cell tumor sphere formation is unaffected. Thus, Sotuletinib hydrochloride has no direct effects on glioma cells, and perturbs macrophage survival through CSF-1R inhibition.
In Vivo: Mice are treated with Sotuletinib hydrochloride or vehicle, and evaluated for symptom-free survival. Median survival in the vehicle-treated cohort is 5.7 weeks. In striking contrast, Sotuletinib hydrochloride significantly improves long-term survival with 64.3% surviving to the 26-week trial endpoint. This endpoint is chosen because Ink4a/Arf?/? mice develop spontaneous tumors, including lymphomas and sarcomas, beginning at ~30 weeks. Sotuletinib hydrochloride is well-tolerated over long-term treatment, with no visible side-effects, consistent with histopathological studies. Histological grading revealed high-grade, invasive gliomas in all vehicle-treated mice. By contrast, Sotuletinib hydrochloride-treated animals have significantly less-malignant tumors, and no detectable lesions in 55.6% of asymptomatic mice at the endpoint. Mice receiving Sotuletinib hydrochloride shows reduced CSF1R staining in both cervical tumors and the associated stroma, with a significant decrease in CSF1R+ stromal macrophages relative to vehicle-treated mice (P<0.05).
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | CSF1R-IN-12 | Pexidartinib | IACS-9439 | Namilumab | AZD7507 | c-Fms-IN-12 | c-Fms-IN-1 | Pazopanib-13C,d3 hydrochloride | Eflapegrastim | Edicotinib | Cabiralizumab | PLX5622 | Otilimab | Plonmarlimab | CSF1R-IN-6 | c-Fms-IN-6 | Linifanib | RET-IN-19 | CSF1R-IN-8 | BPR1R024 mesylate | Lacnotuzumab | cFMS Receptor Inhibitor II | CSF1R-IN-15 | Gimsilumab | Dovitinib-d8 | Vimseltinib | JTE-952 | Axl/Mer/CSF1R-IN-1
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