Stibogluconate sodium

Modify Date: 2024-01-11 10:39:59

Stibogluconate sodium structure	Common Name	Stibogluconate sodium
	CAS Number	16037-91-5	Molecular Weight	910.90
	Density	N/A	Boiling Point	673.6ºC at 760mmHg
	Molecular Formula	C₁₂H₃₈Na₃O₂₆Sb₂	Melting Point	N/A
	MSDS	N/A	Flash Point	375.2ºC

Use of Stibogluconate sodium

Stibogluconate sodium is a potent inhibitor of protein tyrosine phosphatase. Stibogluconate sodium inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.

Name	sodium stibogluconate
Synonym	More Synonyms

Description	Stibogluconate sodium is a potent inhibitor of protein tyrosine phosphatase. Stibogluconate sodium inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase Research Areas >> Cancer
Target	Phosphatase[1]
In Vitro	Stibogluconate sodium inhibits 99% of SHP-1 activity at 10 μg/mL, a therapeutic concentration of the drug for leishmaniasis. Similar degrees of inhibition of SHP-2 and PTP1B required 100 μg/mL Stibogluconate sodium. The inhibition of cellular PTPases by the Stibogluconate sodium is suggested by its rapid induction of tyrosine phosphorylation of cellular proteins in Baf3 cells and its augmentation of IL-3-induced Janus family kinase 2/Stat5 tyrosine phosphorylation and proliferation of Baf3 cells. The augmentation of the opposite effects of GM-CSF and IFN-α on TF-1 cell growth by Stibogluconate sodium indicate its broad activities in the signaling of various cytokines[1].
In Vivo	Stibogluconate sodium induces 61% growth inhibition of Renca tumors in BALB/c mice coincident with an increase (2-fold) in tumor-infiltrating macrophages. A combination of Stibogluconate sodium and IL-2 is more effective in inhibiting tumor growth (91%) and inducing tumor-infiltrating (4-fold), whereas IL-2 alone has little effect[2].
Cell Assay	Human myeloid cell line TF-1 is maintained in RPMI 1640 supplemented with 10% FCS and 40 ng/mL recombinant human GM-CSF. For cell proliferation assays, cells are washed in 10% FCS medium twice, resuspended in 10% FCS medium, incubated at 37°C for 16 h, and then cultured at 37°C in 10% FCS medium containing various amounts of cytokines, sodium stibogluconate, or potassium antimonyl tartrate for 3-6 days. The cell numbers in proliferation assays are determined by an MTT assay or by microscopic cell counting[1].
Animal Admin	BALB/c and athymic nude BALB/c mice are inoculated (s.c.) at the flanks with Renca cells (106 cells/site). Four days after inoculation, the mice are subjected to no treatment (control) or treatment with IL-2 (105 IU/day for 5 days i.p.), Stibogluconate sodium (12 mg/day i.m. at hip regions), or the combination of the two agents for 2 wk. Tumor volume is measured during the study period and calculated using the formula for a prolate spheroid[2].
References	[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.

Boiling Point	673.6ºC at 760mmHg
Molecular Formula	C₁₂H₃₈Na₃O₂₆Sb₂
Molecular Weight	910.90
Flash Point	375.2ºC
PSA	399.06000
Appearance of Characters	solid \| pale yellow
Vapour Pressure	4.95E-21mmHg at 25°C
Water Solubility	H2O: 1 mg/mL at ~75 °C

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

Hazard Codes	Xn,N
Risk Phrases	20/22-51/53
Safety Phrases	61
RIDADR	UN 3282
WGK Germany	3
RTECS	CC7930000
Packaging Group	III
Hazard Class	6.1(b)

1,3,7,9-Tetraoxa-2,8-distibacyclododecane-4,10-dicarboxylic acid, 6,12-bis[(1R)-1,2-dihydroxyethyl]-2,5,8,11-tetrahydroxy-, 2,8-dioxide, sodium salt, (4R,5R,6R,10R,11R,12R)-, hydrate (1:3:9)

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NASBV

Stibogluconate (sodium)