1. Membrane Transporter/Ion Channel
  2. BCRP

Fumitremorgin C (Synonyms: 12α-Fumitremorgin C)

Cat. No.: HY-N2143 Purity: 99.63%
Data Sheet SDS Handling Instructions

Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.

For research use only. We do not sell to patients.
Fumitremorgin C Chemical Structure

Fumitremorgin C Chemical Structure

CAS No. : 118974-02-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO $1878 In-stock
250 ug $160 In-stock
1 mg $450 In-stock
5 mg   Get quote  
10 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.

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 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 IC50 of topotecan in BCRP-overexpressing cells below that observed in the untreated vector-transfected cells. [2].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[1]

Cells are treated with chemotherapeutic agent and the reversal agents Fumitremorgin C is added to cells (0.1 to 80 /UM). In parallel wells, cells are grown in the presence of the reversal agent alone. Following a 3-day growth period, cells are fixed in 10% trichloroacetic acid for 1 h and washed extensively with water, and cell-associated protein is stained using 0.1% SRB. Excess reagent is removed by washing plates in 5% acetic acid, the dye is solubilized in 10 mM Tris base, and absorbance is determined in a UV Max spectrophotometer at 540 nm. Cell survival is determined relative to control wells[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

379.45

Formula

C₂₂H₂₅N₃O₃

CAS No.

118974-02-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Fumitremorgin C
Cat. No.:
HY-N2143
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