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Sotuletinib {[allProObj[0].p_purity_real_show]}

货号:A156169 同义名: BLZ945 Ambeed 开学季,买赠积分,赢豪礼

BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM and > 3200-fold higher than its affinity for other kinases.

Sotuletinib 化学结构 CAS号:953769-46-5
Sotuletinib 化学结构
CAS号:953769-46-5
Sotuletinib 3D分子结构
CAS号:953769-46-5
Sotuletinib 化学结构 CAS号:953769-46-5
Sotuletinib 3D分子结构 CAS号:953769-46-5
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Sotuletinib 纯度/质量文件 产品仅供科研

货号:A156169 标准纯度: {[allProObj[0].p_purity_real_show]}
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Sotuletinib 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].

Sotuletinib 动物研究

Dose Mice: 7 mg/kg - 169 mg/kg[2] (p.o.), 2.5 mg/kg[3] (i.v.) Rat: 10 mg/kg - 150 mg/kg[4] (p.o.) Monkey: 10 mg/kg - 100 mg/kg[4] (p.o.)
Administration p.o., i.v.

Sotuletinib 实验方案

计算器
存储液制备 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

Sotuletinib 技术信息

CAS号953769-46-5
分子式C20H22N4O3S
分子量 398.479
别名 BLZ945
运输蓝冰
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

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