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Sotuletinib hydrochloride

CAS No. : 2222138-31-8

MCE 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).

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