Fumitremorgin C
Based on 3 publication(s) in Google Scholar
Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.92%
- No. CAS: 118974-02-0
- Fòrmula: C22H25N3O3
- Peso molecular:379.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Fumitremorgin C
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.82 nM
Compound: FTC
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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)
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[PMID: 27504669] |
| HEK293 | IC50 |
5.42 nM
Compound: FTC
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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)
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[PMID: 27504669] |
| K562 | IC50 |
41 μM
Compound: 10
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Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
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[PMID: 19256529] |
| NCI-H460 | IC50 |
0.148 μM
Compound: FTC
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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)
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[PMID: 28916341] |
| NCI-H460 | IC50 |
0.168 μM
Compound: FTC
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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)
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[PMID: 28916341] |
| NCI-H460 | IC50 |
0.186 μM
Compound: FTC
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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)
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[PMID: 28916341] |
| NCI-H460 | IC50 |
0.8 μM
Compound: FTC
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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
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[PMID: 21275386] |
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.
Chemical Information
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No. CAS 118974-02-0
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Appearance Solid
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Peso molecular 379.45
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Fòrmula C22H25N3O3
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Color White to off-white
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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
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Synonyms
12α-Fumitremorgin C
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Structure Classification
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Initial Source
Aspergillus fumigatus
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Rabindran SK, et al. Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C. Cancer Res. 1998 Dec 15;58(24):5850-8. [Content Brief]
[2]. Rabindran SK, et al. Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein. Cancer Res. 2000 Jan 1;60(1):47-50. [Content Brief]
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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