Fumitremorgin C是ABCG2/BRCP的选择性抑制剂。
产品描述
Fumitremorgin C is a mycotoxin and inhibits ABCG2/BRCP.
体外活性
Multidrug resistance (MDR) is a major problem in cancer chemotherapy. Reversal of resistance is associated with an increase in drug accumulation. Fumitremorgin C is extremely effective in reversing resistance to mitoxantrone, doxorubicin, and topotecan in multidrug-selected cell lines. Fumitremorgin C reverses mitoxantrone resistance (114-fold) and doxorubicin resistance (3-fold), in MCF-7/mtxR. Fumitremorgin C (5/AM) obviously potentiates the toxicity of doxorubicin (26-fold), mitoxantrone (93-fold), and topotecan (24-fold) in S1M1-3.2 cells. 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 decreases the IC50 of topotecan in BCRP-overexpressing cells below that observed in the untreated vector-transfected cells [2].
Cas No.
118974-02-0
分子式
C22H25N3O3
分子量
379.45
别名
12α-Fumitremorgin C;烟曲霉毒素c
储存和溶解度
DMSO:50 mg/mL (131.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years