Name | Fumitremorgin C |
Synonyms | Fumitremorgin C 12α-Fumitremorgin C 12alpha-Fumitremorgin C FuMitreMorgin CFuMitreMorg Fumitremorgin C, from Aspergillus fumigatus |
CAS | 118974-02-0 |
Molecular Formula | C22H25N3O3 |
Molar Mass | 379.45 |
Density | 1.34±0.1 g/cm3(Predicted) |
Melting Point | 259.5-260.5℃ |
Boling Point | 642.9±55.0 °C(Predicted) |
Solubility | DMSO |
Appearance | solid |
pKa | 17.16±0.40(Predicted) |
Storage Condition | 2-8°C |
In vitro study | Multidrug resistance (MDR) is a major problem in cancer chemotherapy. Fumitremorgin C is extremely effective in reversing resistance to mitoxantrone, doxorubicin, and topotecan in multidrug-selected cell lines. In MCF-7/mtxR (a mitoxantroneselected cell line), fumitremorgin C reverses mitoxantrone resistance (114-fold) and doxorubicin resistance (3-fold). Fumitremorgin C (5/AM)significantly potentiates the toxicity of mitoxantrone (93-fold), doxorubicin (26-fold), and topotecan (24-fold) in S1M1-3.2 cells. Reversal of resistance is associated with an increase in drug accumulation. Fumitremorgin C does not reverse drug resistance in cells with elevated expression of Pgp or MRP. Fumitremorgin C almost completely reverses resistance mediated by BCRP in vitro and is a pharmacological probe for the expression and molecular action of this transporter. Fumitremorgin C also enhances the toxicity of mitoxantrone and topotecan in vector-transfected MCF-7 cells (2.5–5.6 fold). It reduces the IC 50 of topotecan in BCRP-overexpressing cells below that observed in the untreated vector-transfected cells. . |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
Background | Aspergillus fumigatus toxin is produced by Fusarium moniliforme and is commonly found in moldy corn, mycotoxins. Aspergillus fumigatus toxin was found late, the earliest report in 1988, the most common is Aspergillus fumigatus toxin B, Aspergillus fumigatus toxin C. |
biological activity | Fumitremorgin C is a potent, selective inhibitor of ABCG2/BRCP. |