| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
CP-681301 targets cyclin-dependent kinase 5 (Cdk5). It is an ATP-competitive inhibitor that blocks Cdk5 activity. By inhibiting Cdk5, it modulates downstream signaling pathways involved in cell proliferation and survival.
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| ln Vitro |
CP6813101 (1 µM; 96 hours) was found to be cytotoxic to tested GSC cultures in different degrees, but not to NHNPs [1]. The expression of CD133, OLIG2, SOX2, KI67, and pCDK5 protein levels in GSCs is decreased by CP6813101 (0, 10, 50 µM; 48 h) [1]. CP681301 (0.5, 1 µM) suppresses the expression of phosphorylation of CREB Ser133 [1].
In vitro, CP-681301 (5 µM) selectively inhibits Cdk5-dependent proliferation of human medullary thyroid carcinoma (MTC) cells but not normal human fibroblasts. It reduces the expression of CD133, OLIG2, SOX2, KI67, and pCDK5 protein levels in glioblastoma stem cells (GSCs). |
| ln Vivo |
CP681301 (1 mM; fed; 10 days) exhibits antitumor activity in adult Drosophila that are 0 to 2 days old [1].
In vivo, CP-681301 reduces the self-renewal of mouse glioma xenografts. It exhibits anti-tumor activity in Drosophila when administered at 1 mM in the food for 10 days. |
| Enzyme Assay |
In vitro non-cell-based assays for CP-681301 involve measuring its inhibition of Cdk5 kinase activity. The kinase is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound, and the IC50 or Ki is determined.
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| Cell Assay |
Cytotoxicity assay[1]
Cell Types: NHNP, N12.159, GBM121, GBM39, N08-74 Cell Tested Concentrations: 1 µM Incubation Duration: 96 hrs (hours) Experimental Results: demonstrated varying degrees of cytotoxicity to the tested GSC cultures, but not NHNP is not toxic to (normal) human neural progenitor cells). Western Blot Analysis [1] Cell Types: GBM 121, GBM39 Cell Tested Concentrations: 1 µM Incubation Duration: 48 h Experimental Results: Inhibited the expression of CD133, OLIG2, SOX2 and cell proliferation marker KI67. In vitro cell-based assays for CP-681301 are performed in various cancer cell lines, including glioblastoma stem cells (GSCs) and medullary thyroid carcinoma (MTC) cells. Cells are treated with the compound, and cell proliferation, viability, and protein expression are measured. |
| Animal Protocol |
Animal/Disease Models: 0 to 2 days old adult Drosophila (brat-RNAi tumors) [1]
Doses: 1 mM Route of Administration: Fed, 10 days Experimental Results: diminished active phospho-dCdk5 (Y15) in tumor cells, self-renewal capacity Enhanced stem cell properties increased expression of the neuronal marker ElaV in these cells and increased median survival by 2.8-fold. In vivo animal experiments with CP-681301 have been conducted in Drosophila and mouse glioma xenograft models. In Drosophila, the compound is administered in food at 1 mM for 10 days. In mouse models, its effects on tumor growth and self-renewal are assessed. |
| ADME/Pharmacokinetics |
CP-681301 has a molecular weight of 298.38 g/mol and the formula C17H22N4O. It is a solid powder with a purity of ≥98%.
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| Toxicity/Toxicokinetics |
Specific toxicological data for CP-681301 are not detailed in the available literature.
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| References | |
| Additional Infomation |
N-(5-Cyclobutyl-1H-pyrazol-3-yl)-2-(4-(dimethylamino)phenyl)acetamide is an organic molecular entity. It has antitumor activity and is an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor.
CP-681301 is a potent and selective Cdk5 inhibitor. It has shown anti-proliferative and anti-tumor activity in preclinical models. It is intended for research use. |
| Molecular Formula |
C17H22N4O
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|---|---|
| Molecular Weight |
298.382783412933
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| Exact Mass |
298.179
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| CAS # |
865317-32-4
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| PubChem CID |
69763070
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| Appearance |
White to light yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
375
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(CC(NC2C=C(C3CCC3)NN=2)=O)=CC=C(N(C)C)C=C1
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| InChi Key |
PGTNTDKBRSQDNM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H22N4O/c1-21(2)14-8-6-12(7-9-14)10-17(22)18-16-11-15(19-20-16)13-4-3-5-13/h6-9,11,13H,3-5,10H2,1-2H3,(H2,18,19,20,22)
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| Chemical Name |
N-(5-cyclobutyl-1H-pyrazol-3-yl)-2-[4-(dimethylamino)phenyl]acetamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ≥ 100 mg/mL (~335.14 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 | 3.3514 mL | 16.7572 mL | 33.5143 mL | |
| 5 mM | 0.6703 mL | 3.3514 mL | 6.7029 mL | |
| 10 mM | 0.3351 mL | 1.6757 mL | 3.3514 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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