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C0621

CI−994

Name: CI&#8722;994
Brand: SIGMA

≥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:

112522-64-2

分子量:

269.30

UNSPSC Code:

12352200

PubChem Substance ID:

329774808

NACRES:

NA.77

MDL number:

MFCD00866266

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

CI−994, ≥98% (HPLC), powder

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

off-white

solubility

DMSO: >10 mg/mL

storage temp.

room temp

SMILES string

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

Gene Information

human ... HDAC1(3065), HDAC10(83933), HDAC11(79885), HDAC2(3066), HDAC3(8841), HDAC4(9759), HDAC5(10014), HDAC6(10013), HDAC7(51564), HDAC8(55869), HDAC9(9734)

说明

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。

pictograms

GHS07

signalword

Warning

hcodes

H319

pcodes

P264 - P280 - P305 + P351 + P338 - P337 + P313

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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商品

Discover Bioactive Small Molecules for Gene Regulation

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

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)

Gemcitabine plus CI-994 offers no advantage over gemcitabine alone in the treatment of patients with advanced pancreatic cancer: results of a phase II randomized, double-blind, placebo-controlled, multicenter study.

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

Pharmacokinetics and cerebrospinal fluid penetration of CI-994 (N-acetyldinaline) in the nonhuman primate.

L Riva et al.

Clinical cancer research : an official journal of the American Association for Cancer Research, 6(3), 994-997 (2000-03-31)

CI-994 is a substituted benzamide derivative that has demonstrated significant antitumor activity in vitro and in vivo against a broad spectrum of murine and human tumor models. Its mechanism of action is still unknown but seems to be novel compared

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