[CAS NO. 12244-57-4] Aurothiomalate sodium
PRODUCTS SPECIFICATIONS [12244-57-4]
DESCRIPTION [12244-57-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | - |
| Molecular Formula | C4H6O4S.Au.xNa |
| SMILES | OC(CC(S)C(O)=O)=O.[x].[Na].[Au] |
Summary
Aurothiomalate sodium is a potent and selective oncogenic PKC ι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis . Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity [1] [2] [3] .
IC50 & Target
|
PKCι |
In Vitro
Aurothiomalate sodium (0.001, 0.01, 0.1, 1, 10, 100, 1000 uM) induces dose-dependent inhibition of anchorage-independent growth in all cell lines tested (A549, H1437, H2170, H460, H510, H187, H1703 and A427 lung cancer cell lines) with IC
50
s ranging from 300 nM-107 µM. The lung adenocarcinoma (LAC) and small cell lung carcinoma (SCLC) cells tends to be more sensitive and lung adenocarcinomas (LACs) less sensitive to Aurothiomalate sodium
[1]
.
Aurothiomalate sodium (25 uM; 6 hours) suppresses TNFa-induced activation of NF-kB and the expression of NF-kB-targeted proinflammatory genes such as E-selectin and cyclooxygenase-2
[3]
.
Aurothiomalate sodium inhibits non-small lung cancer (NSCLC) growth by binding PKC
ι
and blocking activation of a PKC
ι
-Par6-Rac1-Pak-Mek 1,2-Erk 1,2 signaling pathway
[1]
.
Aurothiomalate sodium inhibits Mek/Erk signaling and decreases proliferative index without effecting tumor apoptosis or vascularization in vivo
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | Bovine arterial endothelial cells (BAEC) |
| Concentration: | 25 uM |
| Incubation Time: | 6 hours |
| Result: |
Suppressed TNFa-induced NF-kB-dependent gene expression in a dose-dependent manner.
Did not affect TrxR1 mRNA level in COS7 cells. |
In Vivo
Aurothiomalate sodium (2, 6, 20 or 60 mg/kg/day; intramuscular injections; 40 days) exhibits statistically significant inhibition of tumor growth at all concentrations tested in A427 cell tumors because A427 cells are highly responsive
[1]
.
Aurothiomalate sodium (20, 60 mg/kg/day; intramuscular injections; 15 days) shows a statistically significant response (~50% reduction in tumor size) only at the 60 mg/kg dose in H460 tumors because H460 cells are less responsive
[1]
.
Aurothiomalate sodium (60 mg/kg/day; IP; for six weeks) exhibites a decrease in tumor growth in Three-week-old KrasLA2 mice. Aurothiomalate sodium inhibits Kras-mediated bronchioalveolar stem cells (BASCs) expansion and lung tumorigenesis in vivo
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 4-6-week-old female nude mice with A427 or H460 cells [1] |
| Dosage: | 2, 6, 20 or 60 mg/kg |
| Administration: | Intramuscular injections; daily; 40 days |
| Result: | Exhibited statistically significant inhibition of tumor growth at all concentrations tested in A427 cell tumors because A427 cells are highly responsive. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 250 mg/mL (Need ultrasonic)
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (Infinity mM); Clear solution; Need ultrasonic
References
- [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.
Synonyms
