C0621
CI−994
≥98% (HPLC), HDAC Inhibitor, powder
别名:
4-乙酰氨基-N-(2′-氨基苯基)苯甲酰胺, 乙酰地那林, 醋地那林
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关于此项目
经验公式(希尔记法):
C15H15N3O2
化学文摘社编号:
分子量:
269.30
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
CI−994, ≥98% (HPLC), powder
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
off-white
溶解性
DMSO: >10 mg/mL
储存温度
room temp
SMILES字符串
CC(=O)Nc1ccc(cc1)C(=O)Nc2ccccc2N
InChI
1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20)
InChI key
VAZAPHZUAVEOMC-UHFFFAOYSA-N
基因信息
应用
CI-994 已用于:
- 作为组蛋白脱乙酰基酶(HDAC)抑制剂,用于处理 SUM229 和 DT22 细胞,以研究其作用
- 作为 HDAC 抑制剂,用在 SPEL 细胞中进行筛选
- 研究其对人类骨髓和红系祖细胞的影响
生化/生理作用
Ci-994 是原始化合物地那林(PD 104 208)的乙酰化衍生物形式。它是一种口服细胞抑制药物,对白血病细胞和正常干细胞的活性差异显著。它用于特定肿瘤的联合治疗,包括非小细胞肺癌、胰腺癌、乳腺癌和结直肠癌。它起组蛋白脱乙酰基酶抑制剂的作用。CI-994 在细胞周期的 G1-S 期阻断细胞。16 kDa 的磷蛋白被限制在核区中。16-kDa 核磷蛋白的丢失似乎是 CI-994 处理的直接效果,并且对该磷蛋白的抑制可能在 CI-994 的作用机理中起关键作用。
口服 HDAC 抑制剂;CI-994 在细胞周期的 G1-S 期阻断细胞。
特点和优势
这种化合物是基因调控研究的特色产品。点击此处发现更多特色基因调控产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
警示用语:
Warning
危险声明
危险分类
Eye Irrit. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
P M LoRusso et al.
Investigational new drugs, 14(4), 349-356 (1996-01-01)
CI-994 [aka: acetyldinaline; PD 123654; 4-acetylamino-N-(2'aminophenyl)-benzamide] (Figure 1) is a novel antitumor agent with a unique mechanism of action. It is the acetylated metabolite of dinaline, a compound previously identified as having cytotoxic and cytostatic activity against several murine and
H M el-Beltagi et al.
Leukemia, 7(11), 1795-1800 (1993-11-01)
The efficacy of acetyldinaline [4-acetylamino-N-(2'-aminophenyl)-benzamide] for eradication of minimal residual disease (MRD), which is left after bone marrow transplantation, and the risk of a bone marrow graft being jeopardized by this treatment was studied in the Brown Norway rat acute
S D Undevia et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 15(11), 1705-1711 (2004-11-03)
This study was conducted to determine the toxicity profile, maximum tolerated dose (MTD) and pharmacokinetics of the putative histone deacetylase inhibitor CI-994 in combination with capecitabine. Fifty-four patients were treated according to three different dosing schemes in which the capecitabine
Ekaterina P Mochalova et al.
Scientific reports, 9(1), 10263-10263 (2019-07-18)
It is known that MuRF-1 and atrogin-1/MAFbx mRNA expression is increased in rat soleus muscle under unloading conditions. We aimed to determine the role of histone deacetylase 1 (HDAC1) in the activation of MuRF-1 and MAFbx expression in rat soleus
The potential role of histone deacetylase inhibitors in the treatment of non-small-cell lung cancer.
Cesare Gridelli et al.
Critical reviews in oncology/hematology, 68(1), 29-36 (2008-04-22)
Non-small-cell lung cancer (NSCLC) arises from a complex series of genetic and epigenetic changes leading to uncontrolled cell growth and metastases. The exponential growth in the level of research about the histone deacetylase (HDAC) enzymes, responsible for deacetylating core nucleosomal
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