葡萄糖酸锑钠

葡萄糖酸锑钠用途

Stibogluconate sodium是蛋白酪氨酸磷酸酶 (phosphatase) 的有效抑制剂。 Stibogluconate sodium在10,100和100 μg/mL时分别抑制99% 的SHP-1,SHP-2和PTP1B活性。

葡萄糖酸锑钠名称

[ CAS 号 ]:
16037-91-5

[ 中文名 ]:
葡萄糖酸锑钠

[ 英文名 ]:
Stibogluconate sodium

[中文别名 ]:

斯锑黑克

[英文别名 ]:

stibanose
stibinol
ANTIMONY SODIUM GLUCONATE
MFCD06795860
solustin
SSG
NASB
stibatin
stibanate
myostibin

葡萄糖酸锑钠生物活性

[ 描述 ]:

Stibogluconate sodium是蛋白酪氨酸磷酸酶 (phosphatase) 的有效抑制剂。 Stibogluconate sodium在10,100和100 μg/mL时分别抑制99% 的SHP-1,SHP-2和PTP1B活性。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸酶

研究领域 >> 癌症

[ 靶点 ]

Phosphatase[1]

[体外研究]

Stibogluconate钠在10μg/ mL时抑制99％的SHP-1活性,这是治疗性利什曼病的药物浓度。 SHP-2和PTP1B的相似程度的抑制需要100μg/ mL的葡萄糖酸盐钠。 Stibogluconate钠对细胞PTP酶的抑制作用表明其快速诱导Baf3细胞中细胞蛋白的酪氨酸磷酸化及其增强IL-3诱导的Janus家族激酶2/Stat5酪氨酸磷酸化和Baf3细胞增殖。 GM-CSF和IFN-α对Stibogluconate钠对TF-1细胞生长的相反作用的增强表明其在各种细胞因子信号传导中的广泛活性[1]。

[体内研究]

Stibogluconate钠诱导BALB/c小鼠中Renca肿瘤的61％生长抑制,与肿瘤浸润性巨噬细胞中的增加(2倍)一致。 Stibogluconate钠和IL-2的组合在抑制肿瘤生长(91％)和诱导肿瘤浸润(4倍)方面更有效,而单独的IL-2几乎没有效果[2]。

[细胞实验]

将人髓样细胞系TF-1维持在补充有10％FCS和40ng / mL重组人GM-CSF的RPMI 1640中。对于细胞增殖测定，将细胞在10％FCS培养基中洗涤两次，重悬于10％FCS培养基中，在37℃下孵育16小时，然后在37℃下在含有不同量细胞因子钠的10％FCS培养基中培养。葡萄糖酸盐或酒石酸锑钾3-6天。增殖测定中的细胞数通过MTT测定或通过显微细胞计数来确定[1]。

[动物实验]

用Renca细胞（106个细胞/位点）在侧腹接种（sc）BALB / c和无胸腺裸BALB / c小鼠。接种后4天，对小鼠进行不处理（对照）或用IL-2处理（105IU /天，腹膜内注射5天），Stibogluconate钠（12mg /天，在臀部区域），或者组合2周的两个特工。在研究期间测量肿瘤体积并使用长椭球体的公式计算[2]。

[参考文献]

[1]. Pathak MK, et al. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001 Sep 15;167(6):3391-7.

[2]. Fan K et al. Sodium Stibogluconate Interacts with IL-2 in Anti-Renca Tumor Action via a T Cell-Dependent Mechanism in Connection with Induction of Tumor-Infiltrating Macrophages. J Immunol. 2005 Nov 15;175(10):7003-8.

[相关活性小分子]

葡萄糖酸锑钠物理化学性质

[ 沸点 ]:
673.6ºC at 760mmHg

[ 分子式 ]:
C₁₂H₃₈Na₃O₂₆Sb₂

[ 分子量 ]:
910.90

[ 闪点 ]:
375.2ºC

[ PSA ]:
399.06000

[ 外观性状 ]:
solid | pale yellow

[ 蒸汽压 ]:
4.95E-21mmHg at 25°C

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

[ 水溶解性 ]:
H2O: 1 mg/mL at ~75 °C

葡萄糖酸锑钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CC7930000

CAS REGISTRY NUMBER :: 16037-91-5

LAST UPDATED :: 199712

DATA ITEMS CITED :: 31

MOLECULAR FORMULA :: C12-H20-O17-Sb2.3Na.9H2-O

MOLECULAR WEIGHT :: 1048.91

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 33 mg/kg

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

REFERENCE :: CLDND* Compilation of LD50 Values of New Drugs. (J.R. MacDougal, Dept. of National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa, Ont., Canada)

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7747 mg/kg

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

REFERENCE :: IJPAAO Indian Journal of Pharmacy. (Bombay, India) V.1-40(1), 1939-78. For publisher information, see IJSIDW. Volume(issue)/page/year: 11,155,1949

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1625 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 18,451,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 77537 mg/kg/30D-I

REFERENCE :: HETOEA Human & Experimental Toxicology. (Macmillan Press Ltd., Brunel Road, Houndmills, Basingstoke, Hampshire, RG21 2XS, UK) V.9- 1990- Volume(issue)/page/year: 11,283,1992 *** REVIEWS *** ACGIH TLV-TWA 0.5 mg(Sb)/m3 DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 TOXICOLOGY REVIEW FAZMAE Fortschritte der Arzneimittelforschung. Progress in Drug Research. (Birkhauser Boston, Inc., c/o Springer-Verlag New York, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1959- Volume(issue)/page/year: 17,108,1973 *** U.S. STANDARDS AND REGULATIONS *** MSHA STANDARD-air:TWA 0.5 mg(Sb)/m3 DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: 3,15,1971 OSHA PEL (Gen Indu):8H TWA 0.5 mg(Sb)/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 29,1910.1000,1994 OSHA PEL (Construc):8H TWA 0.5 mg(Sb)/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 29,1926.55,1994 OSHA PEL (Shipyard):8H TWA 0.5 mg(Sb)/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 29,1915.1000,1993 OSHA PEL (Fed Cont):8H TWA 0.5 mg(Sb)/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 41,50-204.50,1994 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-ARAB Republic of Egypt:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-AUSTRALIA:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-AUSTRIA:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-BELGIUM:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-DENMARK:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-FINLAND:.TWA (0.5 mg(Sb)/m3) JAN 1993 OEL-FRANCE:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-GERMANY:TWA 0.5 mg(Sb)/m3 (total dust) JAN 1993 OEL-HUNGARY:STEL 0.5 mg(Sb)/m3 JAN 1993 OEL-THE NETHERLANDS:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-THE PHILIPPINES:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-POLAND:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-RUSSIA:TWA 0.2 mg(Sb)/m3;STEL 0.5 mg(Sb)/m3 JAN 1993 OEL-SWEDEN:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-SWITZERLAND:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-TURKEY:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL-UNITED KINGDOM:TWA 0.5 mg(Sb)/m3 JAN 1993 OEL IN BULGARIA, COLOMBIA, JORDAN, KOREA check ACGIH TLV OEL IN NEW ZEALAND, SINGAPORE, VIETNAM check ACGIH TLV *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH RECOMMENDED EXPOSURE LEVEL (REL) : NIOSH REL TO ANTIMONY-air:10H TWA 0.5 mg(Sb)/m3 REFERENCE : NIOSH* National Institute for Occupational Safety and Health, U.S. Dept. of Health, Education, and Welfare, Reports and Memoranda. Volume(issue)/page/year: DHHS #92-100,1992

葡萄糖酸锑钠安全信息

[ 危害码 (欧洲) ]:
Xn,N

[ 风险声明 (欧洲) ]:
20/22-51/53

[ 安全声明 (欧洲) ]:
61

[ 危险品运输编码 ]:
UN 3282

[ WGK德国 ]:
3

[ RTECS号 ]:
CC7930000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

葡萄糖酸锑钠制备

葡萄糖酸钙与碳酸钠置换反应生成葡萄糖酸钠，然后用三氯化锑进行锑化反应得到葡萄糖酸三价锑钠盐，最后用双氧水氧化为葡萄糖酸锑钠。