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
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
CI−994, ≥98% (HPLC), powder
SMILES string
CC(=O)Nc1ccc(cc1)C(=O)Nc2ccccc2N
InChI key
VAZAPHZUAVEOMC-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
powder
color
off-white
solubility
DMSO: >10 mg/mL
storage temp.
room temp
Quality Level
Gene Information
Application
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
Biochem/physiol Actions
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。
Features and Benefits
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。
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
D A Richards et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 17(7), 1096-1102 (2006-04-28)
CI-994, an oral histone deacetylase inhibitor, has antineoplastic activity and synergism with gemcitabine preclinically. This randomized phase II trial explored whether CI-994 plus gemcitabine improves overall survival, objective response, duration of response, time to treatment failure and change in quality
CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies
Fuller NO, et al.
ACS Chemical Neuroscience (2019)
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
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
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
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