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Pivanex

Pivanex用途

Pivanex (AN-9) 是丁酸的衍生物,是 HDAC 的抑制剂,具有抗转移和抗血管生成的活性。Pivanex (AN-9) 可下调bcr-abl 蛋白,增强凋亡。

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Pivanex名称

[ CAS 号 ]:
122110-53-6

[ 中文名 ]:
Pivalyloxymethyl butyrate

[ 英文名 ]:
AN-9

[英文别名 ]:

pivaloyloxymethyl butyrate
Pivanex(TM)
((2,2-Dimethylpropanoyl)oxy)methyl butanoate
Pivanex
Pivaloyloxymethyl butyrate Pivanex

Pivanex生物活性

[ 描述 ]:

Pivanex (AN-9) 是丁酸的衍生物,是 HDAC 的抑制剂,具有抗转移和抗血管生成的活性。Pivanex (AN-9) 可下调bcr-abl 蛋白,增强凋亡。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

研究领域 >> 炎症/免疫

信号通路 >> 细胞周期/DNA损伤 >> HDAC

信号通路 >> 表观遗传学 >> HDAC

[体外研究]

Pivanex(100-500μM)对K562细胞具有明显的抗增殖活性[1]。Pivanex(100-500μM)也能增强K562细胞的凋亡和caspase活性[1]。Pivanex(200μM)诱导G2-M期增强,S期中度增强,细胞周期G0-G1轻度减少[1]。Pivanex(AN-9)对急性白血病和耐药的原发性白血病及癌细胞系具有选择性毒性[2]。细胞活力测定[1]细胞系：K562细胞。浓度：100-500μM,培养时间：24小时。结果：K562活细胞数明显减少。100μM Pivanex与0.125或0.25μM STI571协同减少活细胞数。凋亡分析[1]细胞系：K562细胞。浓度：100-500μM,培养时间：6-72小时。结果：K562细胞凋亡明显增多。500μM孵育4h后,K562细胞caspase活性显著升高。

[体内研究]

吡凡尼(AN9 200 mg/kg,b.i.d,每日)显著提高SMN7形状记忆合金小鼠的存活率。AN9治疗也明显延迟了疾病的终末期,正如身体质量损失的开始所定义的那样[3]。动物模型：SMN7 SMA小鼠(SMN2+/+；SMN7+/+；mSmn-/-)[3]。用量：200mg/kg。给药：口服,b.i.d,每日09:00和17:00。结果：治疗组小鼠平均寿命提高84.6%。SMN7 SMA小鼠体重减轻的发生延迟了94.9%。

[参考文献]

[1]. Rabizadeh E, et al. Pivanex, a histone deacetylase inhibitor, induces changes in BCR-ABL expression and when combined with STI571, acts synergistically in a chronic myelocytic leukemia cell line. Leuk Res. 2007 Aug;31(8):1115-23. Epub 2007 Jan 30.

[2]. Batova A, et al. The histone deacetylase inhibitor AN-9 has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines. Blood. 2002 Nov 1;100(9):3319-24.

[3]. Edwards JD, et al. Effect of the Butyrate Prodrug Pivaloyloxymethyl Butyrate (AN9) on a Mouse Model for Spinal Muscular Atrophy. J Neuromuscul Dis. 2016 Nov 29;3(4):511-515.

Pivanex物理化学性质

[ 密度 ]:
1.008g/cm3

[ 沸点 ]:
249.3ºC at 760mmHg

[ 分子式 ]:
C₁₀H₁₈O₄

[ 分子量 ]:
202.24800

[ 闪点 ]:
113ºC

[ 精确质量 ]:
202.12100

[ PSA ]:
52.60000

[ LogP ]:
1.87650

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0231mmHg at 25°C

[ 折射率 ]:
1.43

[ 储存条件 ]:
2-8°C，密封，干燥

PivanexMSDS

详细MSDS(安全技术说明书)

Pivanex毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EK7825000

CHEMICAL NAME :: Butanoic acid, (2,2-dimethyl-1-oxopropoxy)methyl ester

CAS REGISTRY NUMBER :: 122110-53-6

LAST UPDATED :: 199706

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C10-H18-O4

MOLECULAR WEIGHT :: 202.28

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1360 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 35,687,1992

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Pivanex安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

Pivanex文献

A phase I study of pivaloyloxymethyl butyrate, a prodrug of the differentiating agent butyric acid, in patients with advanced solid malignancies.

Clin. Cancer Res. 8(7) , 2142-8, (2002)

Pivaloyloxymethyl butyrate (AN-9), an acyloxyalkyl ester prodrug of butyric acid (BA), has demonstrated greater potency than BA at inducing malignant cell differentiation and tumor growth inhibition a...

Anticancer derivative of butyric acid (Pivalyloxymethyl butyrate) specifically potentiates the cytotoxicity of doxorubicin and daunorubicin through the suppression of microsomal glycosidic activity.

Mol. Pharmacol. 58(1) , 27-36, (2000)

Pivalyloxymethyl butyrate (AN9) is an anticancer derivative of butyric acid. In this study, doxorubicin (DXR) and AN9 synergistically inhibited the growth of lymphoma and lung carcinoma cells, whereas...

Effect of the cytostatic butyric acid pro-drug, pivaloyloxymethyl butyrate, on the tumorigenicity of cancer cells.

J. Cancer Res. Clin. Oncol. 123(5) , 267-71, (1997)

Previously we have shown that pivaloyloxymethyl butyrate (AN-9), a pro-drug of butyric acid (BA), is a differentiation-inducing agent in a variety of cells. In this report, we demonstrate that AN-9 is...

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