| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Cdc7-IN-1 targets Cdc7 kinase (cell division cycle 7), a serine/threonine kinase that plays an essential role in the initiation of DNA replication. Cdc7 phosphorylates the MCM complex (minichromosome maintenance complex), which is required for the activation of replication origins. By inhibiting Cdc7 kinase with an IC50 of 0.6 nM at 1 mM ATP, Cdc7-IN-1 blocks the initiation of DNA replication, leading to cell cycle arrest and apoptosis. The compound's slow off-rate characteristics contribute to its sustained inhibition of Cdc7 activity. Cdc7 is a promising target for cancer therapy, as Cdc7 inhibition selectively induces cell death in cancer cells.
|
|---|---|
| ln Vitro |
Cdc7-IN-1 demonstrates potent in vitro activity as a Cdc7 kinase inhibitor. The compound has an IC50 of 0.6 nM at 1 mM ATP and exhibits slow off-rate characteristics. Its activity is concentration-dependent, with potent inhibition observed at sub-nanomolar concentrations. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells and effectively induces cell death. The compound is an ATP-competitive inhibitor. Its potency and selectivity for Cdc7 make it a valuable tool for studying DNA replication and evaluating Cdc7 inhibition as a therapeutic strategy for cancer.
|
| ln Vivo |
Cdc7-IN-1 has been studied in vivo for its potential as an anticancer agent. The compound potently inhibits Cdc7 activity in cancer cells and effectively induces cell death. Cdc7-IN-1 has anticancer activity. The compound's ability to inhibit Cdc7 in vivo has been demonstrated in preclinical models. Its potency and selectivity for Cdc7 support its potential for cancer research. Comprehensive in vivo efficacy data have been reported in research publications.
|
| Enzyme Assay |
Cdc7-IN-1 is a highly potent, selective, and ATP-competitive inhibitor of Cdc7 kinase, with an IC50 of 0.6 nM at 1 mM ATP and a slow deceleration characteristic.
|
| Cell Assay |
Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death. The compound's slow off-rate characteristics contribute to its sustained inhibition of Cdc7 activity. Each concentration is typically tested in duplicate or triplicate with appropriate positive controls (known Cdc7 inhibitors) and vehicle controls.
|
| Animal Protocol |
In vitro cellular assays for Cdc7-IN-1 are performed using cancer cell lines. Cells are treated with varying concentrations of the compound for defined time periods. Cdc7 kinase activity is assessed by measuring the phosphorylation of its substrate, MCM2, by Western blot using phospho-specific antibodies. Cell proliferation and viability are measured using MTT or CellTiter-Glo assays. Cell cycle analysis is performed by flow cytometry following propidium iodide staining. Apoptosis is measured using annexin V/propidium iodide staining or caspase activity assays. DNA replication can be assessed by measuring [3H]-thymidine incorporation or by using EdU incorporation assays. Cytotoxicity is assessed in parallel to ensure that observed effects are not due to cell death. IC50 values for inhibition of cell proliferation are calculated from dose-response curves.
|
| ADME/Pharmacokinetics |
In vivo animal studies for Cdc7-IN-1 are conducted using mouse xenograft models of cancer. Immunodeficient mice are implanted subcutaneously with cancer cells. Once tumors reach a predetermined size, animals are randomized into treatment groups and administered Cdc7-IN-1 via oral gavage or intraperitoneal injection at various doses and schedules. Tumor growth is measured using calipers. Cdc7 inhibition and apoptosis are assessed in tumor tissues by immunohistochemistry or Western blot. Pharmacokinetic studies assess drug concentrations in plasma and tumor tissues. Animals are monitored for clinical signs and body weight. Efficacy is expressed as tumor growth inhibition compared to vehicle-treated controls.
|
| Toxicity/Toxicokinetics |
Pharmacokinetic properties of Cdc7-IN-1 have been characterized in preclinical studies. The compound has a molecular formula of C21H16ClN3O4 and a molecular weight of 409.82 g/mol. Its chemical name is ethyl 2-[(2-chlorophenyl)amino]-4-oxo-3-[(E)-2-(1H-pyrazolo[3,4-b]pyridin-3-yl)ethenyl]but-2-enoate. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of cancer. Detailed pharmacokinetic data are available from research publications.
|
| References | |
| Additional Infomation |
Cdc7-IN-1 is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As a Cdc7 inhibitor that blocks DNA replication, the compound would be expected to have effects on cell cycle progression and cell division. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound is not approved for human use and is strictly intended for research purposes.
|
| Molecular Formula |
C21H16CLN3O4
|
|---|---|
| Molecular Weight |
409.822443962097
|
| Exact Mass |
409.082
|
| CAS # |
1402055-25-7
|
| PubChem CID |
136230445
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
29
|
| Complexity |
658
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCOC(=O)C1=C(OC(=C1O)/C=C/2\C=NC3=C2C=CC=N3)NC4=CC=CC=C4Cl
|
| InChi Key |
MNEODYFHQBZJNQ-ZRDIBKRKSA-N
|
| InChi Code |
InChI=1S/C21H16ClN3O4/c1-2-28-21(27)17-18(26)16(10-12-11-24-19-13(12)6-5-9-23-19)29-20(17)25-15-8-4-3-7-14(15)22/h3-11,25-26H,2H2,1H3/b12-10+
|
| Chemical Name |
ethyl 2-(2-chloroanilino)-4-hydroxy-5-[(Z)-pyrrolo[2,3-b]pyridin-3-ylidenemethyl]furan-3-carboxylate
|
| 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 : ~5.2 mg/mL (~12.69 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 | 2.4401 mL | 12.2005 mL | 24.4010 mL | |
| 5 mM | 0.4880 mL | 2.4401 mL | 4.8802 mL | |
| 10 mM | 0.2440 mL | 1.2200 mL | 2.4401 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
