产品说明书

Sotuletinib

Print
Chemical Structure| 953769-46-5 同义名 : BLZ945
CAS号 : 953769-46-5
货号 : A156169
分子式 : C20H22N4O3S
纯度 : 99%+
分子量 : 398.479
MDL号 : MFCD28142668
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(213.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

4% DMSO+30% PEG 300+water 2.5 mg/mL

生物活性
描述 The inhibition of CSF-1R, which can deplete macrophages and reduce tumor volume, is an effective strategy to treat for glioblastoma multiforme because of the crucial function of CSF-1R through the paracrine CSF-1–EGF signaling loop in glioma microenvironment forming by the tumor-associated macrophages and microglia (TAMs). BLZ945 is a potent, selective and a brain-penetrant inhibitor of CSF-1R with IC50 value of 1nM (measured by enzymatic activity). The CSF-1–dependent proliferation of wild-type bone marrow–derived macrophages, also pCSF-1R-Y721 induced by CSF-1, can be inhibited by BLZ945 with EC50 value of 67nM. The in vivo study showed that treatment with BLZ945 can substantially decreased microglia numbers in normal brains but not tumor-associated macrophages and microglia in PDGF-B–driven glioma (PDG) mice because of the promotion of TAMs survival by glioma-supplied factors. However, TAMs can be functionally altered in BLZ945 treated gliomas because of the loss of M2 polarization and the enhancement of phagocytosis. Oral dose of 200mg/kg BLZ945 once daily improved survival and decreases glioma malignancy in the transgenic PDG model, with blocking of glioma progression and increased apoptosis[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.25mL

25.10mL

5.02mL

2.51mL