Fumitremorgin C (Synonyms: Tryptoquivaline) |
| Catalog No.GC10874 |
multidrug transporter inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118974-02-0
Sample solution is provided at 25 µL, 10mM.
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Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
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:
[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.
[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.
Cell experiment: | 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]. |
References: [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. | |
| Cas No. | 118974-02-0 | SDF | |
| Synonyms | Tryptoquivaline | ||
| Chemical Name | (5aS,12S,14aS)-9-methoxy-12-(2-methylprop-1-en-1-yl)-1,2,3,5a,6,14a-hexahydropyrrolo[1'',2'':4',5']pyrazino[1',2':1,6]pyrido[3,4-b]indole-5,14(11H,12H)-dione | ||
| Canonical SMILES | O=C([C@H]1N(C2=O)CCC1)N([C@H]3/C=C(C)\C)[C@H]2CC4=C3NC5=C4C=CC(OC)=C5 | ||
| Formula | C22H25N3O3 | M.Wt | 379.45 |
| Solubility | DMSO : 50 mg/mL (131.77 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6354 mL | 13.177 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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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