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| Targets |
CVT-11127 targets SCD1 and IMPDH. It acts as a potent and selective inhibitor of SCD1. It also inhibits IMPDH, a key enzyme in the de novo synthesis of guanine nucleotides. By inhibiting SCD1, it modulates lipid metabolism.
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| ln Vitro |
CVT-11127 (1 µM, 48 hours) displays anti-proliferative action in H460 cells [1]. CVT-11127 (1 µM, 48 hours) lowers the amount of cells in S phase by 75%[1]. CVT-11127 (1 µM, 48 hours) causes apoptosis in H460 cells [1]. CVT-11127 (1, 2 µM) suppresses SCD (stearoyl-CoA desaturase) activity in H460 cells [1].
CVT-11127 reduces cell proliferation in human lung and breast cancer cells. It decreases de novo lipid synthesis from glucose. It impairs the ligand-induced phosphorylation of EGF receptor, causing inactivation of Akt, ERK, and mTOR. It induces apoptosis and arrests the cell cycle at the G1/S phase. |
| ln Vivo |
CVT-11127 has the potential for the research of lung cancer. It reduces cell proliferation and induces apoptosis. It blocks lymphocyte proliferation by inhibiting IMPDH.
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| Enzyme Assay |
CVT-11127 is evaluated in cell-free enzymatic assays using purified SCD1 and IMPDH. The compound is incubated with the enzyme and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of SCD1 and IMPDH inhibition.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: H460 Cell Tested Concentrations: 1 µM Incubation Duration: 48 hrs (hours) Experimental Results: Demonstrated anti-proliferative activity. Cell cycle analysis[1] Cell Types: H460 Cell Tested Concentrations: 1 µM Incubation Duration: 48 hrs (hours) Experimental Results: The number of cells in S phase was diminished by 75%. Apoptosis analysis[1] Cell Types: H460 Cell Tested Concentrations: 1 µM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis in H460 cells. CVT-11127 is assessed in cell-based assays using lung and breast cancer cell lines. Cells are treated with CVT-11127, and cell proliferation, apoptosis, and cell cycle progression are measured. Lipid synthesis and EGF receptor signaling are assessed. |
| Animal Protocol |
CVT-11127 is administered in animal models to evaluate its effects on tumor growth and lipid metabolism. It has been studied in models of lung cancer. Efficacy is assessed by measuring tumor growth inhibition and biomarkers of SCD1 inhibition.
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| ADME/Pharmacokinetics |
CVT-11127 has a molecular weight of 512.39 and a molecular formula of C25H23Cl2N5O3. It has a CAS number of 1018674-83-3. The compound is soluble in DMSO. It should be stored in a cool, dry place.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CVT-11127. The compound is for research use only and is not intended for human therapeutic use. It is a potent SCD1 inhibitor.
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| References | |
| Additional Infomation |
CVT-11127 is a potent and selective SCD1 inhibitor. It also inhibits IMPDH. It induces apoptosis and arrests the cell cycle at the G1/S phase. It is not approved for clinical use.
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| Molecular Formula |
C25H23CL2N5O3
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|---|---|
| Molecular Weight |
512.39
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| Exact Mass |
511.118
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| CAS # |
1018674-83-3
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| PubChem CID |
24830385
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.39±0.1 g/cm3(Predicted)
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| LogP |
4.986
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
776
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)NCCN1C2=C(C=CC(=N2)NCC3=CC(=C(C=C3)Cl)Cl)N=C(C1=O)C4=CC=C(C=C4)OC
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| InChi Key |
PVTIQVJHZDSETN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H23Cl2N5O3/c1-15(33)28-11-12-32-24-21(30-23(25(32)34)17-4-6-18(35-2)7-5-17)9-10-22(31-24)29-14-16-3-8-19(26)20(27)13-16/h3-10,13H,11-12,14H2,1-2H3,(H,28,33)(H,29,31)
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| Chemical Name |
N-[2-[6-[(3,4-dichlorophenyl)methylamino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4-yl]ethyl]acetamide
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| Synonyms |
CVT11127; CVT 11127; CVT-11127
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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 : ~25 mg/mL (~48.79 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 | 1.9516 mL | 9.7582 mL | 19.5164 mL | |
| 5 mM | 0.3903 mL | 1.9516 mL | 3.9033 mL | |
| 10 mM | 0.1952 mL | 0.9758 mL | 1.9516 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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