DS-1205b free base

CAS: 1855860-24-0 货号: D655379 分子式: C41H42FN5O7 分子量: 735.80 PubChem CID: 129110632
有货
级别和纯度: 10mM in DMSO
别名
DS-1205b 游离碱
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
D655379-1ml
期货 Stock Image
¥6,640.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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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


DS-1205b free base is a potent and selective inhibitor of AXL kinase , with an IC 50 of 1.3 nM. DS-1205b free base also inhibits MER , MET , and TRKA , with IC 50 s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo

In Vitro

DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC 50 =2.7 nM). DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI 50 >10,000 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: NIH3T3-AXL cells Concentration: 1, 10, 100, 1000, 10000 μM Incubation Time: 2, 24 hours Result: Completely inhibited the phosphorylation of AXL at concentrations above 10 nM. Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.

In Vivo

DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks Dosage: 3.1, 6.3, 13, 25, 50 mg/kg Administration: P.o. twice daily for 5 days Result: Inhibited tumor growth by 39-94%. Reduced the phosphorylation of both AXL and AKT in tumors.

IC50& Target:AXL 1.3 nM (IC 50 ) MER 63 nM (IC 50 ) TrkA 407 nM (IC 50 ) Met 104 nM (IC 50 )

规格

别名
DS-1205b 游离碱
规格或纯度
10mM in DMSO
英文名称
DS-1205b free base
生化机理
DS-1205b 游离碱是一种强效的 AXL 激酶选择性抑制剂,IC 50 为 1.3 nM。DS-1205b 游离碱还能抑制 MER、MET 和 TRKA,其 IC 50 分别为 63、104 和 407 nM。DS-1205b 游离碱基可抑制维生素 A 诱导的细胞迁移。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
PubChem CID
分子量
735.80

技术文档

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高级数据

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