Adaphostin

• 常用名: Adaphostin
• 英文名: Adaphostin
• CAS号: 241127-58-2
• 分子量: 393.47500
• 密度: 1.33g/cm3
• 沸点: 606.2ºC at 760mmHg
• 分子式: C₂₄H₂₇NO₄
• 熔点: N/A
• 闪点: 320.4ºC

Adaphostin用途

Adaphostin(NSC 680410)是AG957的金刚烷酯,是一种有效的p210bcr/abl抑制剂(IC50=14μM)。阿达磷素诱导T淋巴细胞白血病细胞系(IC50范围为17-216nm)凋亡。阿达磷素对慢性和急性髓系白血病细胞具有显著的选择性活性。阿达磷素增加了CLL B细胞内的活性氧水平[1][2][3]。

Adaphostin名称

• 英文名: 1-adamantyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate

Adaphostin生物活性

• 描述: Adaphostin(NSC 680410)是AG957的金刚烷酯,是一种有效的p210bcr/abl抑制剂(IC50=14μM)。阿达磷素诱导T淋巴细胞白血病细胞系(IC50范围为17-216nm)凋亡。阿达磷素对慢性和急性髓系白血病细胞具有显著的选择性活性。阿达磷素增加了CLL B细胞内的活性氧水平[1][2][3]。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
  信号通路 >> 蛋白酪氨酸激酶 >> BCR-ABL
• 体外研究: 阿达磷素在K562细胞中下调p210bcr/abl,并在低浓度下抑制慢性粒细胞白血病(CML)样本中粒细胞集落形成,而对正常祖细胞没有增强毒性[1]。N-乙酰半胱氨酸(NAC)抑制阿达磷素诱导的ML-1细胞p53上调、DNA链断裂和活性氧生成[4]。
• 参考文献:

  [1]. Svingen PA, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000;6(1):237-249.

  [2]. Avramis IA, et al. In vitro and in vivo evaluations of the tyrosine kinase inhibitor NSC 680410 against human leukemia and glioblastoma cell lines. Cancer Chemother Pharmacol. 2002;50(6):479-489.

  [3]. Orsolic N, et al. Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Cancer Sci. 2006;97(9):952-960.

  [4]. Chandra J, et al. Involvement of reactive oxygen species in adaphostin-induced cytotoxicity in human leukemia cells. Blood. 2003;102(13):4512-4519.

Adaphostin物理化学性质

• 密度: 1.33g/cm3
• 沸点: 606.2ºC at 760mmHg
• 分子式: C₂₄H₂₇NO₄
• 分子量: 393.47500
• 闪点: 320.4ºC
• 精确质量: 393.19400
• PSA: 70.00000
• LogP: 4.99130
• InChIKey: YJZSUCFGHXQWDM-UHFFFAOYSA-N
• SMILES: O=C(OC12CC3CC(CC(C3)C1)C2)c1ccc(NCc2cc(O)ccc2O)cc1
• 蒸汽压: 2.73E-15mmHg at 25°C
• 折射率: 1.661
• 储存条件: -20°C，密封，干燥

Adaphostin安全信息

• 危险品运输编码: NONH for all modes of transport

Adaphostin靶点实验

查看更多实验

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实验名称：uHTS identification of small molecule modulators of NR3A 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：SBCCG-A1015-NR3A-Primary-Assay

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实验名称：MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Activator_SinglePoint... 来源：Broad Institute 靶标：N/A External Id：2084-01_Activator_SinglePoint_HTS_Activity

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Adaphostin英文别名

• tyrphostin AG957 adamantyl ester
• 4'-adamantylbenzoate-1'-N-1,4-dihydroxybenzylamine
• AG 957,Adamantyl Ester
• Adaphostin