CAS NO: | 118974-02-0 |
生物活性 | Fumitremorgin C is a potent and selectiveABCG2/BRCPinhibitor. | ||||||||||||||||
体外研究 (In Vitro) | 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 BCRPin vitroand 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 IC50of topotecan in BCRP-overexpressing cells below that observed in the untreated vector-transfected cells.[2]. | ||||||||||||||||
分子量 | 379.45 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H25N3O3 | ||||||||||||||||
CAS 号 | 118974-02-0 | ||||||||||||||||
结构分类 |
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来源 | Aspergillus fumigatus | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(131.77 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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