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Product Name: AS 101
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106566-58-9

106566-58-9 structure

Name: AS 101
Chemical Name: Ammoniumtrichloro[1,2-ethanediolato-O,O']-tellurate
CAS Number: 106566-58-9
Molecular Formula: C₂H₈Cl₃NO₂Te
Molecular Weight: 312.04900
Catalog: Signaling Pathways Apoptosis Caspase
Create Date: 2017-10-29 21:53:47
Modify Date: 2024-01-11 23:03:31
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor[1]. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies[2][3][4].

Name	Ammoniumtrichloro[1,2-ethanediolato-O,O']-tellurate
Synonyms	AS 101

Description	Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor[1]. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies[2][3][4].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Immunology/Inflammation >> Interleukin Related Signaling Pathways >> Apoptosis >> Caspase Research Areas >> Inflammation/Immunology
Target	IL-1β IL-10 Caspase-1
In Vitro	Ossirene (AS101; 1 μg/mL; for 24 hours) almost completely abrogates expression of pStat3. Ossirene may reduce expression of Bcl-2 after inhibition of Stat3 activation via IL-10 inhibition[2]. AS101 (0.5, 5 mg/mL; 24 hours) inhibits IL-1β-induced mRNA expression of inflammatory mediators in the RPE in a dose-dependent manner. AS101 inhibits IL-1β-induced mRNA expression and protein production of IL-6 and IL-8 in RPE cells. AS101 (5 mg/mL; 1 hour) inhibits the phosphorylation of the p65 component of the NFκB complex activated by IL-1β[1]. Ossirene (0.1, 0.5, 1, 2.5 μg/mL) significantly decreases B16 melanoma, stomach adenocarcinoma, and human glioblastoma multiforme (GBM) cells proliferation[2]. AS101 (0.5 μg/mL; for 24 hours) sensitizes GBM tumor cells to paclitaxel in an IL-10-dependent manner[2]. Western Blot Analysis[2] Cell Line: B16 melanoma cells Concentration: 1 μg/mL Incubation Time: For 24 hours Result: Almost completely abrogated expression of pStat3. RT-PCR[1] Cell Line: ARPE19 cells Concentration: 0.5, 5 mg/mL Incubation Time: 24 hours Result: Inhibited IL-1β-induced mRNA expression of inflammatory mediators in the RPE in a dose-dependent manner.
In Vivo	Ossirene (AS101; 0.5 mg/kg/day; IP; 25 days) sensitizes GBM tumors to paclitaxel via inhibition of IL-10, resulting in increased survival[2]. Animal Model: SCID mice with GBM cells[2] Dosage: 0.5 mg/kg Administration: IP; daily; 25 days Result: Significantly increased survival of GBM tumor-bearing mice.
References	[1]. Diamond Ling, et al. The Tellurium Redox Immunomodulating Compound AS101 Inhibits IL-1β-activated Inflammation in the Human Retinal Pigment Epithelium. Br J Ophthalmol. 2013 Jul;97(7):934-8. [2]. Sredni B, et al. Ammonium trichloro(dioxoethylene-o,o')tellurate (AS101) sensitizes tumors to chemotherapy by inhibiting the tumor interleukin 10 autocrine loop. Cancer Res. 2004 Mar 1;64(5):1843-52. [3]. Yona Kalechman, et al. Inhibition of interleukin-10 by the Immunomodulator AS101 Reduces Mesangial Cell Proliferation in Experimental Mesangioproliferative Glomerulonephritis: Association With Dephosphorylation of STAT3. J Biol Chem. 2004 Jun 4;279(23):24724-32. [4]. Yafit Hachmo, et al. The Small Tellurium Compound AS101 Ameliorates Rat Crescentic Glomerulonephritis: Association With Inhibition of Macrophage Caspase-1 Activity via Very Late Antigen-4 Inactivation. Front Immunol. 2017 Mar 7;8:240.

Density	1.097g/cm3
Boiling Point	197.5ºC at 760mmHg
Molecular Formula	C₂H₈Cl₃NO₂Te
Molecular Weight	312.04900
Flash Point	108.2ºC
Exact Mass	312.86800
PSA	18.46000
LogP	2.01210
Storage condition	-20℃
Water Solubility	Soluble to 5 mM in DMSO and to 5 mM in ethanol

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WY2310000

CHEMICAL NAME :: Tellurate(1-), (1,2-ethanediolato(2-)-O,O')trichloro-, ammonium, (SP-5-22)-

CAS REGISTRY NUMBER :: 106566-58-9

LAST UPDATED :: 199707

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C2-H4-Cl3-O2-Te.H4-N

MOLECULAR WEIGHT :: 312.06

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

REFERENCE :: NICRDR Natural Immunity and Cell Growth Regulation. (S. Karger Publishers, Inc., 79 Fifth Ave., New York, NY 10003 USA) V.3- 1984- Volume(issue)/page/year: 7,163,1988

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

REFERENCE :: NICRDR Natural Immunity and Cell Growth Regulation. (S. Karger Publishers, Inc., 79 Fifth Ave., New York, NY 10003 USA) V.3- 1984- Volume(issue)/page/year: 7,163,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 96 mg/kg/4W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - retinal changes (pigmentary depositions, retinitis, other)

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 17,799,1989

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