Molecular Formula | C72H85N19O18S5 |
Molar Mass | 1664.89 |
Density | 1.0824 (rough estimate) |
Melting Point | 248-257°C (dec.) |
Water Solubility | 0.24g/L(28 ºC) |
Solubility | Soluble in DMSO (10 mg/ml), chloroform (10 mg/ml), dioxane, pyridine, glacial acetic aci |
Appearance | Off-white powder |
Color | Off-white |
Merck | 13,9440 |
pKa | 10.43±0.46(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week. |
Refractive Index | 1.6700 (estimate) |
MDL | MFCD00135828 |
Physical and Chemical Properties | Bioactive Thiostrepton is an antibiotic that selectively inhibits FOXM1. FOXM1 binds to the YAP/TEAD complex. The binding of YAP/TEAD/FOXM1 complex in the gene regulatory region that controls the cell cycle may affect cell proliferation. |
Use | A protein synthesis-inhibiting antibiotic |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
RTECS | XN6300100 |
FLUKA BRAND F CODES | 10-21 |
HS Code | 29419090 |
Toxicity | LD50 oral in mouse: > 1gm/kg |
in vitro studies
Thiostrepton (0.01-1000 μM; 48 hours) suppresses cell viability in A2780 and HEC-1A.
Cell Viability Assay
Cell Line: A2780 and HEC-1A cells
Concentration: 0.01, 0.1, 1, 10, 100, 1000 μM
Incubation Time: 48 hours
Result: The IC 50 s are 1.10 μM in A2780 and 2.22 μM in HEC-1A, respectively.
In vivo studies
Thiostrepton (I .p.; 17 mg/kg) reduces the tumorigenicity of Ewing's sarcoma (EWS) cells. Tumor volumes in control mice have increased ~6-fold from the initiation of treatment, while their Thiostrepton-treated counterparts increase only ~1.7-fold, exhibiting a ~3.5-fold reduction, relative to controls.
Animal Model: Athymic (BALB/c nu/nu) nude mice bearing A4573 cells
Dosage: 17 mg/kg
Administration: Administered I .p.
Result: Treatment inhibited the growth of EWS-derived tumors in vivo.