2. Membrane Transporter/Ion Channel Anti-infection
  3. BCRP Bacterial Antibiotic
  4. Fumitremorgin C

Fumitremorgin C  (Synonyms: 12α-Fumitremorgin C)

Cat. No.: HY-N2143 Purity: 99.90%
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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
250 μg USD 99 In-stock
1 mg USD 286 In-stock
5 mg USD 980 In-stock
10 mg USD 1600 In-stock
25 mg USD 3200 In-stock
50 mg USD 5200 In-stock
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Based on 3 publication(s) in Google Scholar

Fumitremorgin C Related Antibodies

Top Publications Citing Use of Products

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.82 nM
Compound: FTC
Potentiation of mitoxantrone-induced cytotoxicity against HEK293 cells assessed as mitoxantrone IC50 at 3000 nM after 72 hrs by CCK8 assay (Rvb = 1 +/- 0.19 nM)
Potentiation of mitoxantrone-induced cytotoxicity against HEK293 cells assessed as mitoxantrone IC50 at 3000 nM after 72 hrs by CCK8 assay (Rvb = 1 +/- 0.19 nM)
[PMID: 27504669]
HEK293 IC50
5.42 nM
Compound: FTC
Inhibition of human ABCG2 R482 mutant transfected in HEK293 cells assessed as potentiation of mitoxantrone-induced cytotoxicity by measuring mitoxantrone IC50 at 3000 nM after 72 hrs by CCK8 assay (Rvb = 107.40 +/- 13.93 nM)
Inhibition of human ABCG2 R482 mutant transfected in HEK293 cells assessed as potentiation of mitoxantrone-induced cytotoxicity by measuring mitoxantrone IC50 at 3000 nM after 72 hrs by CCK8 assay (Rvb = 107.40 +/- 13.93 nM)
[PMID: 27504669]
K562 IC50
41 μM
Compound: 10
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
[PMID: 19256529]
NCI-H460 IC50
0.148 μM
Compound: FTC
Potentiation of mitoxantrone induced antiproliferative activity against human H460 cells assessed as mitoxantrone IC50 at 10 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 0.215 +/- 0.011 microM)
Potentiation of mitoxantrone induced antiproliferative activity against human H460 cells assessed as mitoxantrone IC50 at 10 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 0.215 +/- 0.011 microM)
[PMID: 28916341]
NCI-H460 IC50
0.168 μM
Compound: FTC
Potentiation of mitoxantrone induced antiproliferative activity against human H460 cells assessed as mitoxantrone IC50 at 3 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 0.215 +/- 0.011 microM)
Potentiation of mitoxantrone induced antiproliferative activity against human H460 cells assessed as mitoxantrone IC50 at 3 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 0.215 +/- 0.011 microM)
[PMID: 28916341]
NCI-H460 IC50
0.186 μM
Compound: FTC
Potentiation of mitoxantrone induced antiproliferative activity against human H460 cells assessed as mitoxantrone IC50 at 1 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 0.215 +/- 0.011 microM)
Potentiation of mitoxantrone induced antiproliferative activity against human H460 cells assessed as mitoxantrone IC50 at 1 uM preincubated for 2 hrs followed by mitoxantrone addition measured after 72 hrs by MTT assay (Rvb = 0.215 +/- 0.011 microM)
[PMID: 28916341]
NCI-H460 IC50
0.8 μM
Compound: FTC
Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C
Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C
[PMID: 21275386]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Fumitremorgin C Related Antibodies
Molecular Weight

379.45

Formula

C22H25N3O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Structure Classification
Initial Source

Aspergillus fumigatus
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (131.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6354 mL 13.1770 mL 26.3539 mL 65.8848 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL 13.1770 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL 6.5885 mL
15 mM 0.1757 mL 0.8785 mL 1.7569 mL 4.3923 mL
20 mM 0.1318 mL 0.6588 mL 1.3177 mL 3.2942 mL
25 mM 0.1054 mL 0.5271 mL 1.0542 mL 2.6354 mL
30 mM 0.0878 mL 0.4392 mL 0.8785 mL 2.1962 mL
40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6471 mL
50 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3177 mL
60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0981 mL
80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
100 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
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Fumitremorgin C Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fumitremorgin C118974-02-012α-Fumitremorgin CBCRPBacterialAntibioticBreast cancer resistance proteinABCG2Inhibitorinhibitorinhibit

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