| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
Nrf2-IN-4 (compound PhcY) (0.01-10 μM, 72 hours) has inhibitory effects on various cancer cell lines, with IC50 values of: MCF-7 cells 80 nM, HepG2 cells 3.26 μM, T24 cells 0.90 μM, HCT116 cells 2.89 μM, L929 fibroblasts 3.27 μM, and HEK293 human embryonic kidney cells 5.36 μM [1]. Nrf2-IN-4 (40-160 nM) can induce MCF-7 cells to exhibit "balloon-like" and round cell morphology, with vacuoles appearing in the cytoplasm [1]. Nrf2-IN-4 (40-80 nM, 14 days) inhibits the clonogenic formation of MCF-7 cells in a dose-dependent manner [1]. Nrf2-IN-4 (80-160 nM, 24-48 h) increases the unstable iron pool (LIP) and induces ferroptosis in MCF-7 cells by inhibiting Nrf2[1]. Nrf2-IN-4 (80-320 nM, 24 h) induces lysosomal activation by promoting the production of iron-dependent reactive oxygen species (ROS) and lysosomal acidification in MCF-7 cells[1]. Nrf2-IN-4 (40-320 nM, 0-12 h) induces ferritin degradation in MCF-7 cells via ferritin autophagy[1]. Nrf2-IN-4 (80-320 nM) induces oxidative stress, resulting in a significant decrease in mitochondrial membrane potential, which can be mitigated by acetylcysteine (N-acetylcysteine) (NAC)[1]. Nrf2-IN-4 (0.1-0.2 μM) showed a strong inhibitory effect on organoid growth, exceeding the efficacy of ML385(3)[1].
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| ln Vivo |
Nrf2-IN-4 (compound PhcY) (10 mg/kg, intraperitoneal injection, once daily for 21 days) showed significant antitumor efficacy in MCF-7 xenograft mice [1].
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| Cell Assay |
Immunofluorescence [1]
Cell Types: MCF-7 cells Tested Concentrations: 80 nM Incubation Duration: 24 hours Experimental Results: LIP increased and Nrf2 knockdown reversed the effect. Cell viability assay [1] Cell Types: MCF-7 cells Tested Concentrations: 80, 160 nM Incubation Duration: 48 hours Experimental Results: Cytotoxicity was enhanced after Nrf2 overexpression. Dose-dependent cytotoxicity was induced, which could be inhibited by 1,8-diazafluorene-9-one (DFO) and Ferrostatin-1 (Fer-1). Immunofluorescence [1] Cell Types: MCF-7 cells Tested Concentrations: 80, 160, 320 nM Incubation Duration: 24 hours Experimental Results: Increased cathepsin B activity in a dose-dependent manner, which could be inhibited by chloroquine (CQ) or deferoxamine (DFO).
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| Animal Protocol |
Animal/Disease Models:MCF-7 cells (5 × 10⁶) were subcutaneously injected into each adult female athymic nude mouse [1].
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection daily for 21 days Experimental Results: Caused degradation of FTH and FTL, and upregulation of P53 and LC3-II expression. No significant weight loss or other observable adverse reactions were observed in mice. |
| References |
| Molecular Formula |
C20H13CL2N5S
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|---|---|
| Molecular Weight |
426.32
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| CAS # |
2417486-06-5
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
ClC1=C(Cl)C=C(C2=CSC(N/N=C(C3=CC=CC=N3)/C4=NC=CC=C4)=N2)C=C1
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3457 mL | 11.7283 mL | 23.4566 mL | |
| 5 mM | 0.4691 mL | 2.3457 mL | 4.6913 mL | |
| 10 mM | 0.2346 mL | 1.1728 mL | 2.3457 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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