计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Sotuletinib (BLZ945) hydrochloride is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC 50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
In Vitro
Sotuletinib hydrochloride inhibits CSF-1-dependent proliferation (EC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
规格
别名
盐酸索妥替尼
规格或纯度
≥98%
英文名称
Sotuletinib hydrochloride
生化机理
索图替尼（BLZ945）盐酸盐是一种强效、选择性和脑穿透性 CSF-1R（c-Fms）抑制剂，IC 50 为 1 nM，对与其最接近的受体酪氨酸激酶同源物的选择性超过 1000 倍。
储存条件
2-8°C储存,干燥
运输条件
低温运输
纯度
≥98%
名称和识别符
分子类型
小分子
Smiles
O=C(C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1)NC.[H]Cl
分子量
434.94
技术文档
高级数据
化学和物理性质
溶解性
H2O : 100 mg/mL (229.92 mM; Need ultrasonic) DMSO : 100 mg/mL (229.92 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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