| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
CPI-4203 targets KDM5A and other KDM5 demethylases. It acts as a selective inhibitor with an IC50 of 250 nM for KDM5A. The compound is competitive with 2-oxoglutarate (2-OG), a co-substrate for the demethylase reaction. By inhibiting KDM5 demethylases, CPI-4203 modulates histone methylation and gene expression.
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|---|---|
| ln Vitro |
In vitro, CPI-4203 acts as a potent KDM5A inhibitor with an IC50 of 250 nM. It is competitive with 2-oxoglutarate. The compound is structurally related to CPI-455 but is less potent. Its activity is typically assessed in enzymatic assays measuring the demethylase activity of KDM5A and related enzymes.
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| ln Vivo |
No specific in vivo activity data is publicly available for CPI-4203. As a research compound targeting epigenetic enzymes, its in vivo efficacy has not been extensively characterized. Further studies would be needed to establish its activity in animal models of cancer or other diseases where KDM5 demethylases play a role.
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| Enzyme Assay |
In cell-free enzymatic assays, CPI-4203's activity is evaluated by measuring its inhibition of KDM5A demethylase activity. The enzyme is incubated with a methylated histone peptide substrate in the presence of varying concentrations of the compound and 2-oxoglutarate. The demethylation of the substrate is measured using techniques such as mass spectrometry or fluorescence-based methods, and the IC50 (250 nM) is calculated.
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| Cell Assay |
In vitro cell-based experiments with CPI-4203 typically involve culturing cancer cell lines and treating them with the compound. The effects on histone methylation levels (e.g., H3K4me3) are measured by Western blot or mass spectrometry. Changes in gene expression are assessed by RNA-seq or qPCR. Cell viability and proliferation assays are used to evaluate the compound's anti-proliferative effects.
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| Animal Protocol |
No specific in vivo animal protocols are publicly available for CPI-4203. If in vivo studies were to be conducted, typical protocols might involve xenograft models in immunodeficient mice, where the compound would be administered, and tumor growth and histone methylation markers would be measured.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CPI-4203. The compound has a molecular formula of C16H14N4O and a molecular weight of 278.31. Its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CPI-4203. As a research compound targeting epigenetic enzymes, its safety profile has not been well established. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
CPI-4203 has a molecular formula of C16H14N4O and a molecular weight of 278.31. It is a selective inhibitor of KDM5 demethylases and a potent KDM5A inhibitor with an IC50 of 250 nM. The compound is competitive with 2-oxoglutarate and is structurally related to CPI-455 but less active. It is available for research purposes only.
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| Molecular Formula |
C16H14N4O
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|---|---|
| Molecular Weight |
278.315
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| Exact Mass |
278.116
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| CAS # |
1628214-07-2
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| PubChem CID |
90442348
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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 |
499.4±55.0 °C at 760 mmHg
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| Flash Point |
255.8±31.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
2.58
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
619
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3C
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| InChi Key |
QMUCSMPNEDSGPT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N4O/c1-3-12-14(13-7-5-4-6-10(13)2)19-15-11(8-17)9-18-20(15)16(12)21/h4-7,9,18H,3H2,1-2H3
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| Chemical Name |
6-ethyl-5-(2-methylphenyl)-7-oxo-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
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| Synonyms |
CPI4203; CPI 4203; CPI-4203
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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 | 3.5930 mL | 17.9649 mL | 35.9299 mL | |
| 5 mM | 0.7186 mL | 3.5930 mL | 7.1860 mL | |
| 10 mM | 0.3593 mL | 1.7965 mL | 3.5930 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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