Sotuletinib,2222138-31-8

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Sotuletinib hydrochloride

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  |  Anti-Blood Cancer Compound Library  |  Membrane Protein-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Cytokine Inhibitors Library  |  Pexidartinib  |  PLX5622  |  Sotuletinib  |  Linifanib  |  Dovitinib  |  GW2580  |  PLX5622 in AIN-76A Diet (1200 ppm)  |  Pazopanib Hydrochloride  |  Edicotinib  |  Vimseltinib  |  Chiauranib  |  PLX647  |  Elzovantinib  |  Seralutinib  |  Emactuzumab  |  PRN1371  |  c-Fms-IN-1  |  Ki20227  |  AZD7507  |  BPR1R024  |  CSF1R-IN-1  |  OSI-930  |  Mavrilimumab  |  cFMS Receptor Inhibitor II  |  CSF1R-IN-3  |  c-Fms-IN-10  |  c-Fms-IN-13  |  c-Fms-IN-8

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds