英文名稱:BLZ945 | CAS:953769-46-5 |
純度規(guī)格: >98% HPLC | 產(chǎn)品類別: 醫(yī)藥級 |
Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs[1].
Treatment of bone marrow-derived macrophages (BMDMs) with Sotuletinib inhibits CSF-1-dependent proliferation (EC50=67 nM), and decreases CSF-1R phosphorylation, similar to CSF-1R antibody blockade. Sotuletinib also reduces viability of CRL-2467 microglia, Ink4a/Arf?/? BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, Sotuletinib 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 has no direct effects on glioma cells, and perturbs macrophage survival through CSF-1R inhibition[1].
Mice are treated with Sotuletinib or vehicle, and evaluated for symptom-free survival. Median survival in the vehicle-treated cohort is 5.7 weeks. In striking contrast, Sotuletinib 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 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-treated animals have significantly less-malignant tumors, and no detectable lesions in 55.6% of asymptomatic mice at the endpoint[1]. Mice receiving Sotuletinib 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)[2].
成立日期 | 2018-07-23 (7年) | 注冊資本 | 100萬 |
員工人數(shù) | 10-50人 | 年營業(yè)額 | ¥ 100萬以內 |
主營行業(yè) | 有機光電,醫(yī)藥中間體,生物活性小分子,原料藥 | 經(jīng)營模式 | 貿易,工廠,試劑,定制,服務 |
產(chǎn)品名稱 | 價格 | 公司名稱 | 報價日期 | |
---|---|---|---|---|
詢價 |
VIP5年
|
上海澤葉生物科技有限公司
|
2024-11-08 | |
詢價 |
VIP8年
|
上海瀚香生物科技有限公司
|
2024-11-08 | |
詢價 |
VIP2年
|
蘇州伽鎂醫(yī)藥科技有限公司
|
2024-11-04 | |
¥700 |
VIP6年
|
無錫東禾醫(yī)藥科技有限公司
|
2024-10-21 | |
詢價 |
VIP6年
|
臺州市科瑞生物技術有限公司
|
2024-09-30 | |
¥269 |
VIP12年
|
上海陶術生物科技有限公司
|
2024-09-24 | |
¥2500 |
VIP10年
|
鹽城康迪森醫(yī)藥科技有限公司
|
2024-09-23 | |
¥974.90 |
VIP1年
|
上海阿拉丁生化科技股份有限公司
|
2024-08-16 | |
詢價 |
VIP2年
|
陜西西化化學工業(yè)有限公司
|
2024-07-24 | |
詢價 |
VIP8年
|
上海瀚香生物科技有限公司
|
2024-11-08 |