| ln Vitro |
Ferroplasm inducer-8 binds to GPX4, reducing the thermal stability of GPX4[1]. Ferroplasm inducer-8 (compound B23) (48 hours) is cytotoxic to tumor cells with IC50 values of: 0.08 μM for MCF-7 cells, 0.04 μM for MDA-MB-231 cells, 0.04 μM for MDA-MB-468 cells, 0.05 μM for HT29 cells, 2.81 μM for A549 cells, 0.06 μM for MPC-3 cells, and 2.23 μM for normal cells (MCF-10A)[1]. Ferroplasm inducer-8 (1 μM, 48 hours) selectively induces ferroptosis in MDA-MB-231 and MDA-MB-468 cells, rather than other cell death mechanisms such as apoptosis, necrosis, or autophagy[1]. Ferroplasmogen-8 (20-60 nM, 7 h) can induce iron metabolism disorder in MDA-MB-231 cells, exacerbate lipid peroxidation, and induce ROS production (10 h) [1]. Ferroplasmogen-8 (20-60 nM, 8 h) can upregulate the expression of ACSL4 in MDA-MB-231 cells and downregulate the expression of FTH1 and GPX4 [1].
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| ln Vivo |
Ferrocyte-induced agent-8 (1–4 mg/kg, intravenous injection, once daily for 21 days) showed antitumor efficacy in the MDA-MB-231 xenograft model [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: MDA-MB-231 and MDA-MB-468 cells Tested Concentrations: 1 μM, co-incubated with Z-VAD-FMK (10 μM), Necrostatin-1 (10 μM) or 3-MA (5 mM); co-incubated with ferroptosis inhibitors Fer-1 (1 μM), DFO (200 μM), GSH (5 mM) or NAC (5 mM) Incubation Duration: Pretreated with various cell death inhibitors for 30 minutes, then co-incubated for 48 hours Experimental Results: Cell viability was inhibited, while Fer-1 ( ), deferoxamine (DFO) ( ), GSH ( ) or NAC ( ) could reverse this inhibition. Z-VAD-FMK ( ), Necrostatin-1 ( ), and 3-MA ( ) could not salvage cytotoxicity. Western Blot Analysis [1] Cell Types: MDA-MB-231 cells Tested Concentrations: 20, 40, 60 nM Incubation Duration: 8 hours Experimental Results: In MDA-MB-231 cells, ACSL4 expression was upregulated, while FTH1 and GPX4 expression was downregulated. Fer-1 (1 μM) could partially restore this regulatory effect. |
| Animal Protocol |
Animal/Disease Models:An MDA-MB-231 xenograft tumor model was established in BALB/c nude mice (4 weeks) [1].
Doses: 1, 2, and 4 mg/kg. Route of Administration: Daily intravenous injection (iv) for 21 consecutive days, at the same dose as above. Experimental Results: Tumor growth was inhibited in a concentration-dependent manner, with a tumor growth inhibition rate (TGI) of 78.46% (4 mg/kg), significantly higher than the positive control group (4 mg/kg RSL3, TGI = 27.21%). At higher doses, toxicity (weight gain) was lower than at RSL3. No significant toxicity to the heart, liver, spleen, lungs, or kidneys was observed (H&E staining). |
| References |
| CAS # |
3097194-74-3
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|---|---|
| Appearance |
Typically exists as solids at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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