1. Membrane Transporter/Ion Channel
  2. BCRP
  3. Fumitremorgin C

Fumitremorgin C (Synonyms: 12α-Fumitremorgin C)

Cat. No.: HY-N2143 Purity: 99.63%
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 USD 1085 In-stock
Estimated Time of Arrival: December 31
250 μg USD 90 In-stock
Estimated Time of Arrival: December 31
1 mg USD 260 In-stock
Estimated Time of Arrival: December 31
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10 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

Molecular Weight

379.45

Formula

C₂₂H₂₅N₃O₃

CAS No.

118974-02-0

SMILES

O=C([[email protected]]1([H])CC2=C([[email protected]](/C=C(C)\C)N13)NC4=C2C=CC(OC)=C4)N5[[email protected]](CCC5)([H])C3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (131.77 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (7.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (7.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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
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