| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
CZC-8004 targets a broad range of tyrosine kinases. By inhibiting these kinases, it disrupts multiple signaling pathways involved in cell proliferation, survival, and migration. Its pan-kinase activity makes it a useful tool for studying kinase signaling networks.
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|---|---|
| ln Vitro |
In vitro, CZC-8004 demonstrates inhibitory activity against a range of tyrosine kinases, including ABL kinase. Specific IC50 values are not widely reported in the available literature.
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| ln Vivo |
In vivo, CZC-8004 is used as a research tool to study kinase signaling pathways. Its pan-kinase activity allows for the investigation of the role of multiple kinases in various biological processes.
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| Enzyme Assay |
The in vitro kinase assay for CZC-8004 involves incubating the enzyme with a peptide substrate and ATP in the presence of varying concentrations of the compound. The amount of phosphorylated substrate is measured using a luminescent or fluorescent detection system, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for CZC-8004 utilize various cancer cell lines. Cells are treated with the compound, and cell viability is assessed by MTT or CellTiter-Glo assays. The phosphorylation of downstream signaling molecules is measured by Western blotting.
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| Animal Protocol |
In vivo animal experiments for CZC-8004 would typically involve xenograft models of cancer. The compound would be administered, and tumor growth would be monitored.
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| ADME/Pharmacokinetics |
CZC-8004 has a molecular weight of 309.34 g/mol and is soluble in DMSO. It is typically stored as a powder at -20°C for up to 3 years. In solution, it is stable at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
Toxicological data for CZC-8004 are limited, as it is a research compound. It is not intended for human use. Standard safety precautions for handling chemical reagents should be followed.
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| References |
CZC-8004 is a pan-kinase inhibitor, with low micromolar IC50 for tyrosine kinase.
[2]. Bantscheff M, et al. Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol. 2007 Sep;25(9):1035-44.
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| Additional Infomation |
CZC8004 is an aminopyrimidine organofluorine compound that acts as a protein kinase inhibitor.
CZC-8004 is a research compound with no clinical approval. It is a valuable tool for studying kinase signaling networks and for exploring the therapeutic potential of multi-kinase inhibitors. |
| Molecular Formula |
C17H16FN5
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|---|---|
| Molecular Weight |
309.3408
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| Exact Mass |
309.138
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| CAS # |
916603-07-1
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| PubChem CID |
15980598
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
514.1±60.0 °C at 760 mmHg
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| Flash Point |
264.7±32.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.699
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| LogP |
2.27
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
342
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UKOHFWNBTUJMMN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16FN5/c18-15-11-20-17(22-14-8-6-12(10-19)7-9-14)23-16(15)21-13-4-2-1-3-5-13/h1-9,11H,10,19H2,(H2,20,21,22,23)
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| Chemical Name |
2-N-[4-(aminomethyl)phenyl]-5-fluoro-4-N-phenylpyrimidine-2,4-diamine
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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 : ~77.5 mg/mL (~250.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.58 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.58 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2327 mL | 16.1634 mL | 32.3269 mL | |
| 5 mM | 0.6465 mL | 3.2327 mL | 6.4654 mL | |
| 10 mM | 0.3233 mL | 1.6163 mL | 3.2327 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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