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| Targets |
The primary target of IZCZ-3 is the c-MYC promoter G-quadruplex structure. By specifically targeting this structure, IZCZ-3 inhibits c-MYC transcription. This leads to decreased cell growth and death. The compound's unique mechanism of action makes it a valuable tool for studying c-MYC-driven cancers.
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| ln Vitro |
The proliferation of SiHa, HeLa, Huh7, and A375 was considerably decreased by IZCZ-3 (2.1 μM-15.9 μM; 24 hours) (IC50 were 3.3, 2.1, 4.1, and 4.2 μM, respectively). In BJ fibroblasts (IC50=15.9 μM) and mouse mesangial cells (IC50=15.6 μM), IZCZ-3 only slightly inhibits proliferation, suggesting that it is more sensitive to humidity than regular IZCZ that isn't dependent on c-MYC. In a dose-dependent manner, -3 (0-5 μM; 12 hours) causes a notable increase of cells in the G0/G1 phase of SiHa cells [1].
In vitro, IZCZ-3 is a potent c-MYC transcription inhibitor. It inhibits c-MYC transcription by specifically targeting the promoter G-quadruplex structure. This leads to decreased c-MYC expression and reduced cell proliferation. Its activity makes it a promising candidate for anticancer research. |
| ln Vivo |
The study examined the tumor growth of fluorescently tagged SiHa human cervical squamous cell carcinoma xenografts in BALB/c nude mice with IZCZ-3 (20, 10, and 5 mg/kg; intraperitoneal basis; once daily for 24 days) [
In vivo, IZCZ-3 inhibits tumor growth in BALB/c nude mice with SiHa human cervical squamous cancer xenografts. This demonstrates its antitumor efficacy in an animal model. Its ability to inhibit c-MYC transcription in vivo makes it a valuable tool for studying c-MYC biology and for developing new cancer therapies. |
| Enzyme Assay |
For c-MYC transcription assays, cells are treated with IZCZ-3, and c-MYC mRNA levels are measured by qRT-PCR. c-MYC protein levels are assessed by Western blot. For G-quadruplex binding assays, the affinity of IZCZ-3 for the c-MYC promoter G-quadruplex can be measured using SPR or fluorescence spectroscopy.
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| Cell Assay |
Cell proliferation analysis [1]
Cell Types: SiHa, HeLa, Huh7 and A375 cancer cells (c-MYC protein overexpression) as well as normal BJ fibroblasts and primary cultured mouse mesangial cells (c-MYC protein expression is relatively Low). Tested Concentrations: 2.1 μM-15.9 μM Incubation Duration: 24 hrs (hours) Experimental Results: The IC50 of SiHa, HeLa, Huh7 and A375 cancer cells were 3.3, 2.1, 4.1 and 4.2 μM respectively; the IC50 of BJ fibroblasts and mouse mesangial cells were respectively 15.9 μM and 15.6 μM. Cell cycle analysis[1] Cell Types: SiHa Cell Tested Concentrations: 0, 1.25, 2.5 and 5 μM Incubation Duration: 12 hrs (hours) Experimental Results: Induced significant accumulation of G0/G1 phase cells (from 61% to 70%) in a dose-dependent manner . For cellular studies, cancer cells are cultured in appropriate medium. IZCZ-3 is dissolved in DMSO and diluted in culture medium. Cells are treated with the compound. Cell viability is assessed by MTT or CellTiter-Glo assays. c-MYC expression is measured by qRT-PCR and Western blot. Cell cycle and apoptosis are analyzed by flow cytometry. |
| Animal Protocol |
Animal/Disease Models: BALB /c nude mice (5 weeks old) SiHa human cervical squamous cell carcinoma xenograft model [1]
Doses: 20, 10, 5 mg/kg Route of Administration: intraperitoneal (ip) injection; 1]. every other day for 24 days Experimental Results: Treatments at 20, 10 and 5 mg/kg resulted in significant reductions in tumor weight, with tumor growth inhibition (TGI) of 69%, 64% and 57%, respectively. Demonstrated time-dependent inhibition of tumor growth. For in vivo efficacy studies, immunodeficient mice are implanted with SiHa cells or other cancer cells. IZCZ-3 is formulated in vehicle and administered intraperitoneally or orally. Tumor growth is monitored. At study termination, tumors are excised and processed for analysis of c-MYC expression, proliferation markers, and apoptosis. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for IZCZ-3 are not extensively reported. As a small molecule, it is expected to have moderate oral bioavailability. Its metabolism likely involves hepatic CYP450 enzymes. A comprehensive PK study would be needed to determine its half-life, Cmax, and AUC for any potential therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for IZCZ-3 are limited. No acute toxicity, organ-specific toxicity, or mutagenicity data have been reported. As with all research compounds, appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
IZCZ-3 (CAS 2223019-53-0) is a potent c-MYC transcription inhibitor with antitumor activity. It targets the c-MYC promoter G-quadruplex. It has the molecular formula C₄₆H₄₉N₇O and a molecular weight of 715.93. It inhibits tumor growth in xenograft models and is strictly for research use.
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| Molecular Formula |
C46H49N7O
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| Molecular Weight |
715.927570104599
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| Exact Mass |
715.399
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| CAS # |
2223019-53-0
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| PubChem CID |
137628645
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| Appearance |
Off-white to pink solid powder
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| LogP |
8.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
54
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C)C1C=CC(=CC=1)N1C(C2C=CC3=C(C=2)C2C=CC=CC=2N3CC)=NC(C2C=CC(=CC=2)N2CCN(C)CC2)=C1C1C=CC(=CC=1)N1CCN(C)CC1
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| InChi Key |
SETZGUYDZNTJCI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C46H49N7O/c1-5-52-42-9-7-6-8-40(42)41-32-35(14-23-43(41)52)46-47-44(33-10-15-36(16-11-33)50-28-24-48(2)25-29-50)45(53(46)38-19-21-39(54-4)22-20-38)34-12-17-37(18-13-34)51-30-26-49(3)27-31-51/h6-23,32H,5,24-31H2,1-4H3
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| Chemical Name |
9-ethyl-3-(1-(4-methoxyphenyl)-4,5-bis(4-(4-methylpiperazin-1-yl)phenyl)-1H-imidazol-2-yl)-9H-carbazole
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| Synonyms |
IZCZ3 IZCZ-3 IZCZ 3
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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 : ~5 mg/mL (~6.98 mM)
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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 | 1.3968 mL | 6.9839 mL | 13.9678 mL | |
| 5 mM | 0.2794 mL | 1.3968 mL | 2.7936 mL | |
| 10 mM | 0.1397 mL | 0.6984 mL | 1.3968 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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