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About This Item
經驗公式(希爾表示法):
C15H15N3O2
CAS號碼:
分子量::
269.30
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
推薦產品
化驗
≥98% (HPLC)
形狀
powder
顏色
off-white
溶解度
DMSO: >10 mg/mL
儲存溫度
room temp
SMILES 字串
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 密鑰
VAZAPHZUAVEOMC-UHFFFAOYSA-N
基因資訊
human ... HDAC1(3065) , HDAC10(83933) , HDAC11(79885) , HDAC2(3066) , HDAC3(8841) , HDAC4(9759) , HDAC5(10014) , HDAC6(10013) , HDAC7(51564) , HDAC8(55869) , HDAC9(9734)
應用
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。
特點和優勢
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。
相關產品
產品號碼
描述
訂價
訊號詞
Warning
危險聲明
危險分類
Eye Irrit. 2
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
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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
M H Seelig et al.
European journal of cancer (Oxford, England : 1990), 32A(11), 1968-1976 (1996-10-01)
Dinaline [4-amino-N-(2'-aminophenyl)-benzamide, Din], p-N-methyldinaline (Me-Din) and p-N-acetyldinaline (Ac-Din) were evaluated for their antineoplastic efficacy in acetoxymethylmethylnitrosamine-induced colorectal carcinomas in Sprague-Dawley rats and in two human colon cancer cell lines. Din was very effective at all dosages (10, 7.7 and 5.9
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 Prakash et al.
Investigational new drugs, 19(1), 1-11 (2001-04-09)
CI-994 (N-acetyl dinaline, PD 123654) is a novel oral agent active in a broad variety of murine and human tumor xenografts. While cytotoxic in the Brown Norway (BN) rat leukemia model, growth inhibition in other murine and human tumor xenografts
文章
Epigenetic modifications are thought to occur through two key interconnected processes—DNA methylation and the covalent modification of histones.
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