| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| 25mg | |||
| Other Sizes |
| Targets |
icFSP1 targets ferroptosis suppressor protein-1 (FSP1), also known as AIFM2 (apoptosis-inducing factor mitochondria-associated 2), which is a key regulator of ferroptosis. FSP1 functions as a glutathione-independent ferroptosis suppressor that reduces coenzyme Q10 to ubiquinol, a lipophilic antioxidant that protects against lipid peroxidation. Unlike competitive inhibitors, icFSP1 does not directly inhibit FSP1 enzyme activity. Instead, it triggers subcellular relocalization of FSP1 from membranes and induces FSP1 condensation prior to ferroptosis induction.
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| ln Vitro |
In vitro, icFSP1 is a potent and selective human FSP1 inhibitor that promotes ferroptosis. The compound does not competitively inhibit FSP1 enzyme activity but instead triggers subcellular relocalization of FSP1 from membranes and FSP1 condensation prior to inducing ferroptosis. icFSP1 acts synergistically with GPX4 inhibition, suggesting that combination therapy targeting both the GPX4 and FSP1 ferroptosis defense pathways may be particularly effective. The compound is soluble in DMSO at 10 mM.
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| ln Vivo |
In vivo activity data for icFSP1 are limited. As a potent FSP1 inhibitor with antitumor activity, the compound is expected to demonstrate efficacy in animal models of cancer by inducing ferroptosis in tumor cells. Typical in vivo studies for FSP1 inhibitors involve administration to tumor-bearing mouse models, with assessment of tumor growth inhibition and ferroptosis biomarkers.
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| Enzyme Assay |
For non-cellular in vitro assays, icFSP1 is evaluated for its effects on FSP1 localization and function using purified FSP1 protein or cell-free systems. The compound's ability to induce FSP1 condensation is assessed using biochemical and biophysical techniques. The compound's lack of competitive inhibition of FSP1 enzyme activity is confirmed by enzyme activity assays that measure FSP1-mediated coenzyme Q10 reduction.
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| Cell Assay |
For in vitro cellular assays, icFSP1 is tested in various cancer cell lines to assess its ability to induce ferroptosis. Cells are treated with serial dilutions of the compound, and ferroptosis is assessed by measuring lipid peroxidation (using C11-BODIPY 581/591 staining), cell viability, and glutathione levels. The compound's synergistic effects with GPX4 inhibitors are evaluated. FSP1 localization and condensation are assessed by immunofluorescence microscopy.
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| Animal Protocol |
For in vivo animal studies, icFSP1 would typically be evaluated in xenograft mouse models of cancer. Mice bearing established tumors are treated with the compound at various doses via intraperitoneal or oral administration. Tumor volumes are measured regularly, and ferroptosis biomarkers (lipid peroxidation, glutathione levels) are assessed in tumor tissues at study endpoint. Body weight and general health are monitored to evaluate tolerability.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for icFSP1 are limited. As a small-molecule inhibitor with a molecular weight of 459.49, it is expected to have moderate oral bioavailability and tissue distribution. The compound is soluble in DMSO at 10 mM and can be formulated for in vivo administration. Further pharmacokinetic studies would be needed to determine its absorption, distribution, metabolism, and excretion profile. The compound is for research use only and not for human use.
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| Toxicity/Toxicokinetics |
Toxicological data for icFSP1 are limited. As a ferroptosis inducer that targets FSP1, the compound may have on-target effects related to FSP1's role in protecting cells from ferroptosis. Comprehensive toxicology studies including acute and repeat-dose toxicity, genotoxicity, and organ-specific toxicity assessments would be required for therapeutic development. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
icFSP1 is a potent and selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor that promotes ferroptosis. Unlike competitive inhibitors, icFSP1 does not inhibit FSP1 enzyme activity but instead triggers subcellular relocalization of FSP1 from membranes and FSP1 condensation prior to inducing ferroptosis. icFSP1 acts synergistically with GPX4 inhibition and is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity. The compound has a molecular weight of 459.49 and molecular formula C₂₆H₂₅N₃O₅.
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| Exact Mass |
459.179
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|---|---|
| CAS # |
1115910-36-5
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| PubChem CID |
46392030
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| Appearance |
White to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
737
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NC2=CC=CC=C2C(=O)N1C3=CC=C(C=C3)NC(=O)CC4=CC(=C(C(=C4)OC)OC)OC
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| InChi Key |
QLTZGMMQMVZODD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H25N3O5/c1-16-27-21-8-6-5-7-20(21)26(31)29(16)19-11-9-18(10-12-19)28-24(30)15-17-13-22(32-2)25(34-4)23(14-17)33-3/h5-14H,15H2,1-4H3,(H,28,30)
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| Chemical Name |
N-[4-(2-methyl-4-oxoquinazolin-3-yl)phenyl]-2-(3,4,5-trimethoxyphenyl)acetamide
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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: ~100 mg/mL (~217.6 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.44 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 2.5 mg/mL (5.44 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
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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