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| 化学名: | タセジナリン | | 英語化学名: | Tacedinaline | | 别名: | Benzamide, 4-(acetylamino)-N-(2-aminophenyl)-;Tacedinaline;CI 994;N-Acetyldinaline;4-AcetaMido-N-(2-aMinophenyl)benzaMide;Cl-994(Tacedinalin,N-Acetyldinalin);CI994 (Tacedinaline);CI-994 4-Acetylamino-N-(2'-aminophenyl)benzamide | | CAS番号: | 112522-64-2 | | 分子式: | C15H15N3O2 | | 分子量: | 269.3 | | EINECS: | 200-256-5 | | カテゴリ情報: | Inhibitors;Inhibitor;Apoptosis Inducers | | Mol File: | 112522-64-2.mol |  |
| 融点 | 216.1 °C | | 沸点 | 450.6±30.0 °C(Predicted) | | 比重(密度) | 1.322±0.06 g/cm3(Predicted) | | RTECS 番号 | CU8702023 | | 貯蔵温度 | Keep in dark place,Inert atmosphere,2-8°C | | 溶解性 | Soluble in DMSO | | 酸解離定数(Pka) | 13.15±0.70(Predicted) | | 外見 | powder | | 色 | off-white | | Sensitive | Air Sensitive | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. | | InChIKey | VAZAPHZUAVEOMC-UHFFFAOYSA-N |
| 主な危険性 | Xi | | Rフレーズ | 36 | | Sフレーズ | 26 | | WGK Germany | 3 | | HSコード | 2924.29.7790 |
| | タセジナリン Usage And Synthesis |
| 外観 | うすい黄赤色～黄色～緑色粉末～結晶 | | 効能 | 抗悪性腫瘍薬, ヒストン脱アセチル化酵素阻害薬 | | 説明 | CI-994 (112522-64-2) is an orally active histone deacetylase (HDAC) inhibitor, IC50 = 0.9, 0.9, 1.2 and >20 μM for HDAC1, HDAC2, HDAC3 and HDAC8 respectively.1 Mediates G1 cell cycle arrest, inhibits proliferation and induces apoptosis in vitro and in vivo.2,3 Increases neuroplasticity during memory extinction.4 Protects beta cells from cytokine-induced apoptosis.4 | | 使用 | Tacedinaline is a histone deacetylase (HDAC) inhibitor. Tacedinaline is an anti-cancer agent as HDAC inhibitors block angiogenesis, arrest cell growth, and lead to differentiation and apoptosis in tumor cells. Studies show Tacedinaline to be effective against acute myeloid leukemia in vitro and in vivo when used in combination with conventional anti-cancer agents. | | 使用 | Tacedinaline is a histone deacetylase (HDAC) inhibitor. Tacedinaline is an anti-cancer agent as HDAC inhibitors block angiogenesis, arrest cell growth, and lead to differentiation and apoptosis in tum
or cells. Studies show Tacedinaline to be effective against acute myeloid leukemia in vitro and in vivo when used in combination with conventional anti-cancer agents. | | 定義 | ChEBI: A benzamide obtained by formal condensation of the carboxy group of 4-acetamidobenzoic acid with one of the amino groups of 1,2-phenylenediamine. An oral cytostatic drug with impressive differential activity against leukemic cells and normal stem-cells. Al
o used in combination therapy for selected tumors including non-smoll cell lung, pancreatic, breast, and colorectal cancers. | | 生物活性 | Orally active histone deacetylase (HDAC) inhibitor (K i values are 0.41, 0.75, >100 and >100 μ M for HDAC1, HDAC3, HDAC6 and HDAC8 respectively). Mediates G 1 cell cycle arrest, inhibits proliferation and induces apoptosis in vitro and in vivo . | | target | HDAC1 | | 貯蔵 | +4°C | | 参考文献 | 1) Moradei et al. (2007), Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity; J. Med. Chem., 50 5543
2) Beckers et al. (2007), Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group; Int. J. Cancer, 121 1138
3) Loprevite et al. (2005), In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines; Oncol. Res., 15 39
4) Chou et al. (2012), Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis; Chem. Biol., 19 669 |
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