| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
ZIM targets DNA, acting as a potent inducer of DNA damage. Its mechanism of action involves breaking the DNA molecule, which leads to genomic and chromosomal instability. This DNA damage subsequently triggers cellular responses such as cell death and activates phagocytosis. The compound's chemotherapeutic potential is directly related to its ability to induce this DNA damage.
|
|---|---|
| ln Vitro |
In vitro studies confirm ZIM's activity as a DNA damage inducer. It causes genomic and chromosomal damage in cellular models. The compound's ability to break DNA molecules and induce cell death has been demonstrated, establishing its potential as a chemotherapeutic agent. Its activity is often assessed by measuring the extent of DNA fragmentation or chromosomal aberrations in treated cells.
|
| ln Vivo |
ZIM (ip, 12, 24, and 48 mg/kg) has a certain chemopreventive effect, lowers the spectrum of damage by percentage, and effectively lowers chromosomal micronucleus frequency at all dosages at 24 and 72 hours in adult male Swiss mice. between 38.36 and 83.26%[1]. ZIM (ip, 12, 24, and 48 mg/kg) can lessen the frequency of doxorubicin-DOX and cisplatin-CIS-induced liver and kidney cell death. The percentages of liver damage decrease in the CIS group were 79.27, 75.20, and 52.84% at dose concentrations of 12, 24, and 48 mg/kg, while the percentages in the DOX group were 62.06, 59.44, and 77.80%. For the CIS group, the reduction in kidney damage was 45.29, 36.09, and 41.61%; for the DOX group, it was 28.00, 21.41, and 30.82% [1].
In vivo activity of ZIM has been evaluated in adult male Swiss mice. Intraperitoneal (i.p.) administration of ZIM at doses of 12, 24, and 48 mg/kg effectively reduced the frequency of chromosomal micronuclei, with the percentage of damage reduction ranging from 38.36% to 83.26%. Furthermore, ZIM was shown to reduce the frequency of cisplatin- and doxorubicin-induced liver and kidney cell death. For instance, in the cisplatin group, liver damage reduction was between 52.84% and 79.27%, while in the doxorubicin group, it ranged from 59.44% to 77.80%. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays are not the primary method for characterizing ZIM's activity, as its mechanism is based on direct DNA interaction rather than binding to a specific enzyme or receptor. Its activity is assessed by evaluating its ability to induce DNA damage. This is typically measured using techniques like the comet assay, which quantifies DNA strand breaks, or by assessing the formation of micronuclei as an indicator of chromosomal damage.
|
| Cell Assay |
In vitro cellular assays for ZIM involve treating cultured cancer cells with the compound and then assessing the extent of DNA damage and cell death. These assays typically measure DNA fragmentation, chromosomal aberrations, or cell viability. The induction of phagocytosis can also be evaluated by assessing the uptake of apoptotic cells by macrophages.
|
| Animal Protocol |
In vivo animal experiments for ZIM have been conducted in mouse models. In these studies, ZIM is typically administered via intraperitoneal (i.p.) injection. The primary endpoints for evaluating its efficacy include the reduction of chromosomal damage (measured by micronucleus frequency) and the mitigation of chemotherapy-induced organ toxicity in the liver and kidneys. The compound's chemopreventive effects and its impact on the DNA damage spectrum are also assessed in these models.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for ZIM are not detailed in the provided sources. The compound has a molecular weight of 349.38 and a LogP of 2.1. It is available as a solid powder. For research purposes, it is typically dissolved in DMSO. The compound is intended for research use only, and comprehensive ADME data are not available.
|
| Toxicity/Toxicokinetics |
Toxicological data for ZIM are derived from in vivo studies. While it induces DNA damage, it has also been shown to reduce the toxicity caused by chemotherapeutic agents like cisplatin and doxorubicin in the liver and kidneys of mice. This suggests a potential chemopreventive effect alongside its DNA-damaging activity. At the tested doses (12-48 mg/kg in mice), it demonstrated efficacy in reducing chromosomal damage.
|
| References |
[1]. Rodrigo Juliano Oliveira, et al. ZIM, a Norbornene Derived from 4-Aminoantipyrine, Induces DNA Damage and Cell Death but in Association Reduces the Effect of Commercial Chemotherapeutics. Chem Res Toxicol. 2022 Dec 22.
|
| Additional Infomation |
ZIM (CAS#: 301298-87-3) is a norbornene derivative of 4-Aminoantipyrine and a potent DNA damage inducer. It is used in cancer research to study the effects of genomic instability and to explore its potential as a chemotherapeutic agent. Interestingly, ZIM also exhibits chemopreventive properties by reducing the organ toxicity associated with other chemotherapeutics. The compound's purity is typically ≥98%.
|
| Molecular Formula |
C20H19N3O3
|
|---|---|
| Molecular Weight |
349.38
|
| Exact Mass |
349.14
|
| CAS # |
301298-87-3
|
| PubChem CID |
5096714
|
| Appearance |
Solid powder
|
| LogP |
2.1
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
26
|
| Complexity |
734
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(=O)C2C(C3CC2C=C3)C(=O)N1C1=C(C)N(C)N(C2=CC=CC=C2)C1=O
|
| InChi Key |
QOOKFECIGXERRL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H19N3O3/c1-11-17(20(26)23(21(11)2)14-6-4-3-5-7-14)22-18(24)15-12-8-9-13(10-12)16(15)19(22)25/h3-9,12-13,15-16H,10H2,1-2H3
|
| Chemical Name |
4-(1,5-dimethyl-3-oxo-2-phenylpyrazol-4-yl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione
|
| Synonyms |
ZIM
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~143.1 mM)
|
|---|---|
| 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 | 2.8622 mL | 14.3111 mL | 28.6221 mL | |
| 5 mM | 0.5724 mL | 2.8622 mL | 5.7244 mL | |
| 10 mM | 0.2862 mL | 1.4311 mL | 2.8622 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05633667 | Recruiting | Drug: Zimberelimab (ZIM) Drug: Carboplatin |
Advanced or Metastatic Non- Small-Cell Lung Cancer |
Gilead Sciences | March 16, 2023 | Phase 2 |
| NCT02038335 | Completed | Drug: DMPA Drug: NET-EN |
HIV Microbiota |
University of Pittsburgh | February 2014 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
