基本信息

技术规格

物性(参考值)

安全信息

图形或危害标志
信号词	警告
危险性说明	H341 : 怀疑可造成遗传性缺陷。
防范说明	P501 : 将内装物/容器送到批准的废物处理厂处理。 P202 : 在阅读并明了所有安全措施前切勿搬动。 P201 : 使用前取得专用说明。 P280 : 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P308 + P313 : 如接触到或有疑虑：求医/就诊。 P405 : 存放处须加锁。

相关法规

基本信息

产品描述

Decitabine是DNA甲基转移酶抑制剂，整合进入DNA、导致DNA低甲基化，并使DNA复制停滞在intra-S-phase。Decitabine被用于治疗骨髓增生异常综合征(MDS）。

靶点（IC50 & Targe）

DNA methyltransferase (DNMT)

体外研究

Decitabine 有效抑制DNA 合成，这种作用存在剂量依赖性，作用于HL-60和 KG1a 白血病细胞时，IC50分别为 100 ng/mL 和1 ng/mL。Decitabine 抑制细胞生长，这种作用存在剂量和时间依赖性，处理HL-60和KG1a白血病细胞72小时和96小时，IC50分别约为100 ng/mL 和 10 ng/mL。[1] 最新研究显示Decitabine作用于间变性大细胞淋巴瘤(ALCL)，具有抗增殖和促凋亡活性，且抑制KARPAS-299细胞中[3H]胸甘的摄取，EC50 为0.49 μM。[2]

体内研究

Decitabine 按2.5 mg/kg 剂量作用于ALK+ KARPAS-299小鼠移植瘤模型，促进凋亡，且降低肿瘤细胞增殖，也导致肿瘤抑制基因p16INK4A的去甲基化。 [2]

激酶实验

DNA合成检测 :

通过测定放射性胸甘摄入到DNA的情况而测定DNA合成比率。HL-60 和KG1a 细胞悬浮在6孔(直径为35 mm )盘中，孔中为含10%胎牛血清的2 mL RPMI 培养基中,然后与不同浓度相应药物温育48小时 (药物同时加入)。48小时时, 每孔加入0.5 μCi [3H] 胸甘(6.7 Ci/mmol)，再温育24小时。细胞置于GF/C玻璃纤维过滤器(直径为2.4 cm)中，使用冷 0.9% NaCl, 5% 冷三氯乙酸和乙醇清洗。烘干含DNA的过滤器，置于EcoLite闪烁液(ICN)中，使用 Beckman LS 6000IC 闪烁计数器测量放射性。通过剂量-反应曲线计算IC50值。

细胞实验

Cell lines: HL-60 和 KG1a

Concentrations: 0 到100 ng/mL

Incubation Time: 96 小时

Method: 生长抑制实验中，指数生长期细胞接种在5 ml培养基中。向培养基中同时加入不同浓度Decitabine。在指定时间，使用模型 ZM Coulter 计数器对细胞进行计数。根据药物处理的白血病细胞的生长曲线，测定IC50值。

(Only for Reference)

动物实验

Animal Models: KARPAS-299 人类细胞皮下接种到小鼠的左右两侧。

Formulation: Decitabine 溶于无菌PBS

Dosages: ≤2.5 mg/kg

Administration: 腹腔注射

(Only for Reference)

参考文献

[1] Shaker S, et al. Leuk Res, 2003, 27(5), 437-444.

[2] Hassler MR, et al. Biochimie, 2012, doi.org/10.1016/j.biochi.

安全信息

图形或危害标志
提示语	Danger
危险说明	H302 H315 H319 H335 H341 H360
防范说明	P201 P261 P281 P305+P351+P338 P308+P313
WGK	3
RTECS	XZ3012000

产品说明

一般描述

A cytosine analog that acts as a DNA methyltransferase inhibitor. Shown to restore mRNA and protein expression of caspase-8 and Tumor Necrosis Factor-Related Apoptosis Inducing Ligand (TRAIL) sensitivity of resistant cell lines. Also reported to enhance apoptosis induced by histone deacetylase (HDAC) inhibitors.
A cytosine analog that acts as a DNA methyltransferase inhibitor. Restores caspase-8 and caspase-10 mRNA and protein expression as well as TRAIL (Tumor necrosis factor-Related Apoptosis Inducing Ligand) sensitivity in TRAIL-resistant cell lines. Also enhances apoptosis induced by HDAC (Histone Deacetylase) inhibitors. Also available as a 100 mM solution in DMSO (Cat. No. 189826).

包装

25 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Primary Target
DNA methyltransferase inhibitor

警告

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

制备说明

warming is required to achieve complete solubilization

重悬

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Eggert, A., et al. 2001. Cancer Res.61, 1314.
Takebayashi, S., et al. 2001. Biochem. Biophys. Res. Commun.288, 921.
Zhu, W.G., et al. 2001. Cancer Res.61, 1327.
Hopkins-Donaldson, S., et al. 2000. Cancer Res.60, 4315.
Haaf, T. 1995. Pharmacol. Ther.65, 19.
Jones, P.A., and Taylor, S.M. 1980. Cell20, 85.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H302 - H315 - H319 - H335 - H341 - H360
预防措施声明	P201 - P202 - P301 + P312 - P302 + P352 - P305 + P351 + P338 - P308 + P313
危险分类	Acute Tox. 4 Oral - Eye Irrit. 2 - Muta. 2 - Repr. 1B - Skin Irrit. 2 - STOT SE 3
靶器官	Respiratory system
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3

产品说明

一般描述

5-氮杂-2′-脱氧胞苷是一种DNA次甲基化剂，可刺激白血病细胞分化和凋亡。它是一种2′-脱氧胞苷类似物。5-氮杂-2′-脱氧胞苷用于治疗慢性粒细胞单核细胞白血病、难治性贫血、骨髓增生异常综合症和急性髓细胞性白血病。

应用

5-氮杂-2′-脱氧胞苷已被用作乳腺癌细胞系、染色质、DNA和p16基因启动子区域的脱甲基剂。

包装

5, 10 mg in glass bottle
50 mg in glass insert

生化/生理作用

5′-脱氧杂氮胞苷可引起DNA去甲基化或半去甲基化。DNA去甲基化可通过随着提高的核酸酶活性而“打开”染色质的结构来调控基因的表达。这种染色质结构的重塑可实现转录因子与启动子区域的结合、转录复合物的组装及基因表达。地西他滨是一种表观遗传修饰因子，可抑制DNA甲基转移酶活性而重塑“开放的”染色质，导致DNA去甲基化(低甲基化)和基因活化。当去甲基化与组蛋白超乙酰化组合时，基因会被协同重新激活。

特点和优势

该化合物是基因调控研究的特色产品。点击此处以了解更多的基因调控特色产品。可访问sigma.com/discover-bsm了解更多关于用于其他研究领域生物活性小分子。
该化合物由Eisai开发。如需浏览其他药物开发的化合物和批准的药物/候选药物清单，请单击此处。

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H302 - H315 - H319 - H335 - H341 - H360
预防措施声明	P201 - P301 + P312 + P330 - P302 + P352 - P305 + P351 + P338 - P308 + P313
危险分类	Acute Tox. 4 Oral - Eye Irrit. 2 - Muta. 2 - Repr. 1B - Skin Irrit. 2 - STOT SE 3
靶器官	Respiratory system
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
个人防护装备	dust mask type N95 (US), Eyeshields, Gloves

产品说明

一般描述

A cytosine analog that acts as a DNA methyltransferase inhibitor. Restores caspase-8 and caspase-10 mRNA and protein expression as well as TRAIL (Tumor necrosis factor-Related Apoptosis Inducing Ligand) sensitivity in TRAIL-resistant cell lines. Also enhances apoptosis induced by HDAC (Histone Deacetylase) inhibitors. The solid form of this compound (Cat. No. 189825) is also available.

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

外形

A 100 mM (10 mg/438 µl) solution of 5-Aza-2ʹ-Deoxycytidine (Cat. No. 189825) in DMSO.

其他说明

Eggert, A., et al. 2001. Cancer Res.61, 1314.
Takebayashi, S., et al. 2001. Biochem. Biophys. Res. Commun.288, 921.
Zhu, W.G., et al. 2001. Cancer Res.61, 1327.
Hopkins-Donaldson, S., et al. 2000. Cancer Res.60, 4315.
Haaf, T. 1995. Pharmacol. Ther.65, 19.
Jones, P.A., and Taylor, S.M. 1980. Cell20, 85.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

基本信息

安全信息

图形或危害标志
危险性说明	H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation. H341: Suspected of causing genetic defects .. H360: May damage fertility or the unborn child ..
防范说明	P201: Obtain special instructions before use. P202: Do not handle until all safety precautions have been read and understood. P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing P264: Wash hands thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P281: Use personal protective equipment as required. P301 + P312: IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: . P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P308 + P313: IF exposed or concerned: Get medical advice/ attention. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see . on this label). P330: Rinse mouth. P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to local regulations.