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羟基硫胺素盐酸盐

羟基硫胺素盐酸盐用途

盐酸羟硫胺(羟硫胺)是抗代谢产物的类似物,可抑制核糖的非氧化合成并诱导细胞凋亡。盐酸氧硫胺素是一种硫胺素拮抗剂,可抑制转酮酶(TK)。盐酸氧硫胺抑制癌症细胞凋亡并抑制细胞增殖[1][2][3]。

羟基硫胺素盐酸盐名称

[ CAS 号 ]:
614-05-1

[ 中文名 ]:
羟基硫胺素盐酸盐

[ 英文名 ]:
Oxythiamine chloride hydrochloride

[中文别名 ]:

羟基硫胺盐酸盐

[英文别名 ]:

OXYTHIAMINE CHLORIDE HCL
MFCD00050656

羟基硫胺素盐酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

[ 靶点 ]

Vitamin B1, Thiamine, Transketolase[1].

[体外研究]

盐酸氧噻嗪(0-40μM,2天) 抑制迈阿密PaCa-2细胞的细胞活力(IC50:14.95μM)[1]盐酸氧噻嗪(0-500μM,48小时) 抑制迈阿密PaCa-2细胞中 14-3-3 蛋白 β/α的表达[1]。盐酸氧硫胺素(0.1-100μM,6-48小时)抑制第549页细胞增殖[3]. 盐酸氧硫胺素(0.1-100μM,24小时)诱导第549页细胞凋亡[3]. [3]. 盐酸氧噻嗪(0-20μM)抑制刘易斯肺癌 (LLC)细胞的侵袭和迁移 (IC50:8.75μM)[4]细胞活力测定[1]细胞系：MIA PaCa-2细胞浓度：0-40μM培养时间：2天结果：抑制细胞活力,IC50为14.95μM。Western Blot分析[1]细胞系：MIA PaCa-2细胞浓度：0、5、50、500μM培养时间：48小时结果：抑制14-3-3蛋白β/α表达,并增加α烯醇化酶。

[体内研究]

盐酸氧噻嗪(100-500 mg/kg,i.p.4天) 抑制艾氏腹水瘤宿主小鼠的肿瘤生长[2]。盐酸氧噻嗪(250或 500mg/kg每日一次,持续 5.周) 通过抑制植入 (皮下)有限责任公司细胞的小鼠体内的 MMP来抑制肿瘤细胞转移[4]。动物模型：艾氏腹水瘤宿主小鼠[2]剂量：100-500 mg/kg给药：腹腔注射,4天结果：300 mg/kg时抑制肿瘤生长43%,500 mg/kg时抑制84%。

[参考文献]

[1]. Wang J, et al. Inhibition of transketolase by oxythiamine altered dynamics of protein signals in pancreatic cancer cells. Exp Hematol Oncol. 2013 Jul 27;2:18.

[2]. Raïs B, et al. Oxythiamine and dehydroepiandrosterone induce a G1 phase cycle arrest in Ehrlich's tumor cells through inhibition of the pentose cycle. FEBS Lett. 1999 Jul 30;456(1):113-8.

[3]. Bai L, et al. A dose- and time-dependent effect of oxythiamine on cell growth inhibition in non-small cell lung cancer. Cogn Neurodyn. 2022 Jun;16(3):633-641.

[4]. Yang CM, et al. The in vitro and in vivo anti-metastatic efficacy of oxythiamine and the possible mechanisms of action. Clin Exp Metastasis. 2010 May;27(5):341-9.

羟基硫胺素盐酸盐物理化学性质

[ 分子式 ]:
C₁₂H₁₆Cl₂N₄O₂S

[ 分子量 ]:
351.25200

[ 精确质量 ]:
350.03700

[ PSA ]:
107.56000

[ 储存条件 ]:
-20°C，密闭，干燥

羟基硫胺素盐酸盐MSDS

详细MSDS(安全技术说明书)

羟基硫胺素盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ7034100

CHEMICAL NAME :: Thiazolium, 3-((1,4-dihydro-2-methyl-4-oxo-5-pyrimidinyl)methyl)- 5-(2-hydroxyethyl)-4- methyl-, chloride, monohydrochloride

CAS REGISTRY NUMBER :: 614-05-1

LAST UPDATED :: 199707

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C12-H16-N3-O2-S.Cl.Cl-H

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 1835 mg/kg

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

REFERENCE :: VMDKAM Voprosy Meditsinskoi Khimii. Problems of Medical Chemistry. (V/O Me zhdunarodnaya Kniga, 113095 Moscow, USSR) V.1- 1955- Volume(issue)/page/year: 33,70,1987

羟基硫胺素盐酸盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ RTECS号 ]:
XJ7034100

[ 海关编码 ]:
2934100090

羟基硫胺素盐酸盐合成路线

详细合成路线

羟基硫胺素盐酸盐上下游产品

羟基硫胺素盐酸盐上游产品

羟基硫胺素盐酸盐下游产品

羟基硫胺素盐酸盐海关

[ 海关编码 ]: 2934100090

[ 中文概述 ]:
2934100090. 结构上含有一个非稠合噻唑环的化合物(不论是否氢化). 增值税率:17.0%. 退税率:9.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

羟基硫胺素盐酸盐文献

Inhibition of protein phosphorylation in MIA pancreatic cancer cells: confluence of metabolic and signaling pathways.

J. Proteome Res. 9 , 980-989, (2010)

Oxythiamine (OT), a transketolase inhibitor, is known to inhibit pancreatic cancer cell proliferation. In this study, we investigated the effect of inhibition of the transketolase pathway on signaling...

The in vitro and in vivo anti-metastatic efficacy of oxythiamine and the possible mechanisms of action.

Clin. Exp. Metastasis 27 , 341-349, (2010)

This study examined the anti-metastatic effects of oxythiamine (OT) both in cell culture and in vivo. Cell culture results revealed that OT (0-20 microM) significantly inhibited the invasion and migra...

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