TASP0415914

• 常用名: TASP0415914
• 英文名: TASP0415914
• CAS号: 1292300-75-4
• 分子量: 323.37100
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₃H₁₇N₅O₃S
• 熔点: N/A
• 闪点: N/A

TASP0415914用途

TASP0415914是一种有效的口服活性PI3Kγ抑制剂,IC50为29 nM。TASP0415914还显示出强大的Akt抑制活性,IC50为294nm。TASP0415914可用于炎症性疾病研究[1]。

TASP0415914名称

• 英文名: N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide

TASP0415914生物活性

• 描述: TASP0415914是一种有效的口服活性PI3Kγ抑制剂,IC50为29 nM。TASP0415914还显示出强大的Akt抑制活性,IC50为294nm。TASP0415914可用于炎症性疾病研究[1]。
• 相关类别:
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> AKT
  研究领域 >> 炎症/免疫
• 靶点实验:

  PI3Kγ:29 nM (IC50)

  Akt:294 nM (IC50)

• 体外研究: TASP0415914(化合物8j)在大鼠/人肝微粒体中显示出高代谢稳定性。TASP0415914对CYP1A2、2C9、2C19、2D6和3A4在10μM以下没有CYP抑制作用[1]。
• 体内研究: TASP0415914(化合物8j；10-100mg/kg；口服给药；每日两次；在小鼠胶原诱导关节炎(CIA)模型中,14天的治疗以剂量依赖性方式抑制疾病的进展[1]。动物模型：胶原诱导的DBA/1小鼠[1]剂量：10mg/kg；30mg/kg；100mg/kg给药：口服给药；每日两次；14天结果：以剂量依赖性方式抑制疾病进展。
• 参考文献:

  [1]. Yusuke Oka, et al. Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases. Bioorg Med Chem. 2013 Dec 15;21(24):7578-83.

TASP0415914物理化学性质

• 分子式: C₁₃H₁₇N₅O₃S
• 分子量: 323.37100
• 精确质量: 323.10500
• PSA: 132.62000
• LogP: 1.55900
• InChIKey: WFQFHKQIDOCQTL-UHFFFAOYSA-N
• SMILES: CC(=O)Nc1nc(C)c(-c2nc(N3CCCC(O)C3)no2)s1
• 储存条件: 2-8°C，干燥，密封

TASP0415914安全信息

• 危害码 (欧洲): Xi

TASP0415914靶点实验

查看更多实验

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实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Mutagenicity in Salmonella typhimurium TA98 up to 5000 ug/ml by Ames test in presence... 来源：ChEMBL 靶标：Salmonella enterica subsp. enterica serovar Typhimurium External Id：CHEMBL3097337

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

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