MDL | - |
---|---|
Molecular Weight | 379.45 |
Molecular Formula | C22H25N3O3 |
SMILES | O=C([C@]1([H])CC2=C([C@H](/C=C(C)\C)N13)NC4=C2C=CC(OC)=C4)N5[C@](CCC5)([H])C3=O |
Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
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 [1] . 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. [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Aspergillus fumigatus
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 50 mg/mL ( 131.77 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.6354 mL | 13.1770 mL | 26.3539 mL |
5 mM | 0.5271 mL | 2.6354 mL | 5.2708 mL |
10 mM | 0.2635 mL | 1.3177 mL | 2.6354 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 3 mg/mL (7.91 mM); Clear solution