金(I)硫丁二酸钠_MSDS_用途_分子量_CAS号【12244-57-4】

金硫代苹果酸钠是一种有效和选择性的致癌PKCι信号抑制剂。硫代硫酸亚金钠抑制肿瘤细胞增殖而不是细胞凋亡。硫代硫酸亚金钠是一种有效的硫氧还蛋白还原酶(TrxR)抑制剂。金硫代苹果酸钠是一种抗类风湿药物,具有强大的抗肿瘤活性[1][2][3]。

[ 描述 ]:

金硫代苹果酸钠是一种有效和选择性的致癌PKCι信号抑制剂。硫代硫酸亚金钠抑制肿瘤细胞增殖而不是细胞凋亡。硫代硫酸亚金钠是一种有效的硫氧还蛋白还原酶(TrxR)抑制剂。金硫代苹果酸钠是一种抗类风湿药物,具有强大的抗肿瘤活性[1][2][3]。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 癌症

研究领域 >> 炎症/免疫

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

PKCι

[体外研究]

金硫代苹果酸钠(0.001,0.01,0.1,1,10,100,1000μM)诱导所有受试细胞系(A549、H1437、H2170、H460、H510、H187、H1703和A427肺癌细胞系)中锚定非依赖性生长的剂量依赖性抑制,IC50范围为300 nM-107µM。肺腺癌(LAC)和小细胞肺癌(SCLC)细胞对金硫代苹果酸钠更敏感,而肺腺癌(LAC)对金硫代苹果酸钠更不敏感[1]。碘酸亚金钠(25μm；6小时)抑制TNFa诱导的NF-κB活化和NF-κB靶向促炎基因如E-选择素和环氧合酶-2的表达[3]。金硫代苹果酸钠通过结合PKCι并阻断PKCι-Par6-Rac1-Pak-Mek 1,2-Erk 1,2信号通路的激活来抑制非小肺癌(NSCLC)的生长[1]。金硫代苹果酸钠抑制Mek/Erk信号传导,降低增殖指数,但不影响体内肿瘤细胞凋亡或血管形成[1]。westernblot分析[1]细胞系：牛动脉内皮细胞(BAEC)浓度：25μm孵育时间：6小时结果：以剂量依赖性方式抑制TNFa诱导的NF-kB依赖性基因表达。不影响COS7细胞中TrxR1 mRNA水平。

[体内研究]

硫代硫酸亚金钠(2、6、20或60 mg/kg/天；肌肉注射；在A427细胞肿瘤中测试的所有浓度下,由于A427细胞具有高度反应性,因此在统计上显著抑制肿瘤生长[1]。硫代硫酸亚金钠(20,60 mg/kg/天；肌肉注射；在H460肿瘤中,仅在60 mg/kg剂量下显示出统计上显著的反应(肿瘤大小减少约50%),因为H460细胞的反应性较低[1]。硫代硫酸亚金钠(60毫克/千克/天；知识产权；六周)表明三周龄KrasLA2小鼠的肿瘤生长减少。碘酸金钠抑制体内Kras介导的支气管肺泡干细胞(BASC)扩增和肺肿瘤发生[2]。动物模型：4-6周龄雌性裸鼠,A427或H460细胞[1]剂量：2、6、20或60 mg/kg给药：肌肉注射；每日的40天结果：在A427细胞肿瘤的所有测试浓度下显示出统计上显著的肿瘤生长抑制,因为A427细胞具有高度的反应性。

[参考文献]

[1]. Roderick P Regala, et al. Atypical protein kinase C iota expression and aurothiomalate sensitivity in human lung cancer cells. Cancer Res. 2008 Jul 15;68(14):5888-95.

[2]. Roderick P Regala, et al. Atypical protein kinase C{iota} is required for bronchioalveolar stem cell expansion and lung tumorigenesis. Cancer Res. 2009 Oct 1;69(19):7603-11.

[3]. Atsuko Sakurai, et al. Overexpression of thioredoxin reductase 1 regulates NF-kappa B activation. J Cell Physiol. 2004 Jan;198(1):22-30.

[ 分子式 ]:
C₄H₃AuNa₂O₄S

[ 分子量 ]:
390.07500

[ 精确质量 ]:
389.92100

[ PSA ]:
105.56000

[ 储存条件 ]:
室温，密封，干燥

[ 水溶解性 ]:
Very soluble in water. Practically insoluble in alcohol, ether

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MD5435000

CHEMICAL NAME :: Gold, ((1,2-dicarboxyethyl)thio)-, disodium salt

CAS REGISTRY NUMBER :: 12244-57-4

LAST UPDATED :: 199504

DATA ITEMS CITED :: 30

MOLECULAR FORMULA :: C4-H3-Au-O4-S.2Na

MOLECULAR WEIGHT :: 390.08

WISWESSER LINE NOTATION :: OVYVO&1S-AU- &-NA- 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5500 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - recording from peripheral motor nerve Kidney, Ureter, Bladder - renal function tests depressed Blood - thrombocytopenia

REFERENCE :: ARHEAW Arthritis and Rheumatism. (Arthritis Foundation, 1314 Spring St., NW, Atlanta, GA 30309) V.1- 1958- Volume(issue)/page/year: 19,936,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 182 ug/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,1294,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2700 ug/kg/4W-I

TOXIC EFFECTS :: Brain and Coverings - changes in circulation (hemorrhage, thrombosis, etc.)

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 11,235,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 20 mg/kg/1Y

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - aggression Kidney, Ureter, Bladder - proteinuria

REFERENCE :: ARPAAQ Archives of Pathology. (Chicago, IL) V.5(3)-50(3), 1928-50; V.70-99, 1960-75. For publisher information, see APLMAS. Volume(issue)/page/year: 96,133,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5 mg/kg/13W

TOXIC EFFECTS :: Blood - hemorrhage Blood - thrombocytopenia Musculoskeletal - changes in teeth and supporting structures

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 133,754,1947

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 600 ug/kg/1W-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - fibrosis (interstitial) Liver - jaundice, cholestatic Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: JRSMD9 Journal of the Royal Society of Medicine. (Oxford Univ. Press, Walton St., Oxford OX2 6DP, UK) V.71- 1978- Volume(issue)/page/year: 77,960,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3366 ug/kg/2W

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - muscle weakness

REFERENCE :: NEURAI Neurology. (Modern Medicine Pub., Inc., 1 E. First St., Duluth, MN 55802) V.1- 1951- Volume(issue)/page/year: 20,455,1970

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 12500 ug/kg/7W-I

TOXIC EFFECTS :: Brain and Coverings - encephalitis Peripheral Nerve and Sensation - fasciculations Peripheral Nerve and Sensation - structural change in nerve or sheath

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 11,233,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7857 ug/kg/11W-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Immunological Including Allergic - uncharacterized

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 286,1547,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 11900 ug/kg/18W-I

TOXIC EFFECTS :: Biochemical - Metabolism (Intermediary) - other

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 13,224,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human

DOSE/DURATION :: 9750 ug/kg/23W-I

TOXIC EFFECTS :: Blood - changes in cell count (unspecified) Blood - aplastic anemia Blood - other changes

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,1266,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 12 mg/kg

TOXIC EFFECTS :: Blood - thrombocytopenia

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 13,225,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1600 ug/kg/3W-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), diffuse Blood - agranulocytosis

REFERENCE :: ANZJB8 Australian and New Zealand Journal of Medicine. (Modern Medicine of Australia Pty., Ltd., 100 Pacific Highway, North Sydney, 2060, Australia) V.1- 1971- Volume(issue)/page/year: 16,72,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 7 mg/kg/7W-I

TOXIC EFFECTS :: Blood - thrombocytopenia

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 12,180,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7857 ug/kg/11W-I

TOXIC EFFECTS :: Immunological Including Allergic - uncharacterized

REFERENCE :: BJRHDF British Journal of Rheumatology. (Bailliere Tindall, 33 The Avenue, Eastborn BN21 3UN, UK) Volume(issue)/page/year: 24,367,1985

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 303 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,208,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 440 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,208,1982

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 185 mg/kg

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

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 49,121,1942

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 930 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,208,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 855 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,208,1982

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 800 mg/kg

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

REFERENCE :: VTPHAK Veterinary Pathology. (Waverly Press, Inc., POB 64025, Baltimore, MD 21264) V.8- 1971- Volume(issue)/page/year: 15(Suppl 5),1,1978 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 75 mg/kg

SEX/DURATION :: female 4-6 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 214,250,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 75 mg/kg

SEX/DURATION :: female 13-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 214,250,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 250 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: VTPHAK Veterinary Pathology. (Waverly Press, Inc., POB 64025, Baltimore, MD 21264) V.8- 1971- Volume(issue)/page/year: 15(Suppl 5),89,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 100 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: CBINA8 Chemico-Biological Interactions. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1969- Volume(issue)/page/year: 58,149,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 900 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

REFERENCE :: VTPHAK Veterinary Pathology. (Waverly Press, Inc., POB 64025, Baltimore, MD 21264) V.8- 1971- Volume(issue)/page/year: 15(Suppl 5),89,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 257 mg/kg

SEX/DURATION :: female 6-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: VTPHAK Veterinary Pathology. (Waverly Press, Inc., POB 64025, Baltimore, MD 21264) V.8- 1971- Volume(issue)/page/year: 15(Suppl 5),97,1978 *** REVIEWS *** TOXICOLOGY REVIEW MDCHAG Medicinal Chemistry: A Series of Monographs. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1963- Volume(issue)/page/year: 13(1),209,1974 TOXICOLOGY REVIEW PTPAD4 Pharmacology and Therapeutics, Part A: Chemotherapy, Toxicology and Metabolic Inhibitors. (Oxford, UK) V.1-2, 1976-78. For publisher information, see PHTHDT. Volume(issue)/page/year: 1,119,1976 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6050 No. of Facilities: 14 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 731 (estimated) No. of Female Employees: 366 (estimated)

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R20/21/22;R43

[ 安全声明 (欧洲) ]:
S36

[ WGK德国 ]:
3

[ RTECS号 ]:
MD5435000

[ 海关编码 ]:
2930909090

[ 海关编码 ]: 2930909090

[ 中文概述 ]:
2930909090. 其他有机硫化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Sodium aurothiomalate

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥2701.0/1g ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：阿拉丁李高志

产品详情：硫代苹果酸金钠

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金(I)硫丁二酸钠物理化学性质