AS 101

Modify Date: 2025-08-27 11:41:53

AS 101 Structure
AS 101 structure
Common Name AS 101
CAS Number 106566-58-9 Molecular Weight 312.04900
Density 1.097g/cm3 Boiling Point 197.5ºC at 760mmHg
Molecular Formula C2H8Cl3NO2Te Melting Point N/A
MSDS N/A Flash Point 108.2ºC

 Use of AS 101


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].

 Names

Name Ammoniumtrichloro[1,2-ethanediolato-O,O']-tellurate
Synonym More Synonyms

 AS 101 Biological Activity

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
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.

 Chemical & Physical Properties

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

 Toxicological Information

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

 Synonyms

AS 101
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