| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| ln Vitro |
In cancer chemotherapy, multidrug interactions (MDR) represent a significant challenge. In multidrug-selected cell lines, fumiremorgin C is incredibly successful in reversing the interaction of mitocinone, doxorubicin, and topotecan. Fugitremorgin C reversed doxorubicin-quinone selectivity (3-fold) and mitoxantrone-quinone selectivity (114-fold) in MCF-7/mtxR, a mitoxantrone-selected cell line. In S1M1-3.2 cells, fumiremorgin C (5/AM) markedly increased the toxicity of mitoxantrone (93-fold), doxorubicin (26-fold), and topotecan (24-fold). reversal of the activity in cells expressing MRP or Pgp at high levels [1]. Fumitremorgin C is a pharmacological marker of the expression and molecular function of this transporter, and it almost entirely recovers BCRP-mediated interactions in vitro. Additionally, mitoxantrone and topotecan were 2.5–5.6 times more lethal to vector-transfected MCF-7 cells when fumiremorgin C was present. At that point, untreated vector-transfected cells' IC50 for topotecan decreased to a value lower than that of BCRP-overexpressing cells [2].
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| Toxicity/Toxicokinetics |
Toxicity Summary
Fumartramokinen C inhibits the ATP-binding cassette transporter (ACBG2), also known as the breast cancer resistance protein. ACBG2 is known to confer multidrug resistance and affect the bioavailability of various drugs. Therefore, fumaromokinen C is often used to enhance the sensitivity of cancer patients to chemotherapy drugs. Tremor-inducing fungal toxins exert their toxic effects by interfering with neurotransmitter release, possibly by causing nerve ending degeneration. They are thought to inhibit presynaptic and postsynaptic γ-aminobutyric acid (GABA) receptors and inhibit neurotransmitter degradation at GABA-T receptors. This initially leads to elevated neurotransmitter levels, enhancing GABA-induced chloride ion currents, and then resulting in decreased neurotransmitter levels at the synapse. (A2974, A2975, A2976, A3027) |
| References | |
| Additional Infomation |
Aspergillus Fumitremorgin C is an organic heteropentacyclic compound belonging to the fungal toxin indole alkaloids produced by various fungi. It is a potent and specific inhibitor of multidrug transporters for breast cancer resistance proteins. It is both a fungal toxin and an inhibitor of breast cancer resistance proteins. It is an indole alkaloid, an organic heteropentacyclic compound, and an aromatic ether. Aspergillus Fumitremorgin C has been reported to be found in Aspergillus ferruginea, Aspergillus Fumitremorgin, and other organisms with relevant data. Both Aspergillus Fumitremorgin and Neosatolaxii produce aspergillus Fumitremorgin C.
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| Molecular Formula |
C22H25N3O3
|
|---|---|
| Molecular Weight |
379.4522
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| Exact Mass |
379.189
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| CAS # |
118974-02-0
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| PubChem CID |
403923
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
642.9±55.0 °C at 760 mmHg
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| Melting Point |
259.5-260.5℃
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| Flash Point |
342.6±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
|
| Index of Refraction |
1.676
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| LogP |
1.74
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
28
|
| Complexity |
703
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| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC(=C[C@H]1C2=C(C[C@@H]3N1C(=O)[C@@H]4CCCN4C3=O)C5=C(N2)C=C(C=C5)OC)C
|
| InChi Key |
DBEYVIGIPJSTOR-FHWLQOOXSA-N
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| InChi Code |
InChI=1S/C22H25N3O3/c1-12(2)9-18-20-15(14-7-6-13(28-3)10-16(14)23-20)11-19-21(26)24-8-4-5-17(24)22(27)25(18)19/h6-7,9-10,17-19,23H,4-5,8,11H2,1-3H3/t17-,18-,19-/m0/s1
|
| Chemical Name |
(1S,12S,15S)-7-methoxy-12-(2-methylprop-1-enyl)-10,13,19-triazapentacyclo[11.7.0.03,11.04,9.015,19]icosa-3(11),4(9),5,7-tetraene-14,20-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~131.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (7.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (7.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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