| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In a panel of colorectal cancer (CRC) cell lines, the CDK5 inhibitor 20-223 (10 nM-10 μM; 72 h) efficiently reduces cell proliferation [1]. Three CRC cell lines were treated at reduced doses with CDK5 inhibitor 20-223 (0.3125 – 20,000 μM; 6 h) to induce pRB (S807/811) and pFAK (S732) levels [1].
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|---|---|
| ln Vivo |
In human colorectal cancer xenograft tumors in nude mice, the CDK5 inhibitor 20-223 (8 mg/kg; subcutaneous injection; 14 injections) demonstrated tumor anti-tumor efficacy [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: CRC cell line SW620, DLD1, HT29, HCT116, FET, CBS and GEO Cell Tested Concentrations: 10 μM, 1 μM, 100 nM, 10 nM Incubation Duration: 72 hrs (hours) Experimental Results: diminished cell growth. The IC50 of SW620, DLD1, HT29, HCT116, FET, CBS and GEO cells were 168±20, 480±41, 360±72, 763±92, 117±49, 568±49, 79±31 nM. Western Blot Analysis[1] Cell Types: CRC cell lines GEO, HCT116 and HT29 Tested Concentrations: 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM Incubation Duration: 6 hrs (hours) Experimental Results: Did not affect total levels of CDK2/5, and Levels of total FAK or total retinoblastoma protein (Rb). A dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels was induced. |
| Animal Protocol |
Animal/Disease Models: athymic nude mice [1]
Doses: 8 mg/kg Route of Administration: subcutaneous injection every day in the first week, subcutaneous injection every other day for two weeks, a total of 14 injections. Experimental Results: In vivo tumor growth and tumor weight were diminished. |
| References |
| Molecular Formula |
C19H19N3O
|
|---|---|
| Molecular Weight |
305.373664140701
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| Exact Mass |
305.152
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| CAS # |
865317-30-2
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| PubChem CID |
69761759
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
423
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CC1C=C2C(C=CC=C2)=CC=1)NC1C=C(C2CCC2)NN=1
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| InChi Key |
AGVIDDQHAQSPIZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19N3O/c23-19(20-18-12-17(21-22-18)15-6-3-7-15)11-13-8-9-14-4-1-2-5-16(14)10-13/h1-2,4-5,8-10,12,15H,3,6-7,11H2,(H2,20,21,22,23)
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| Chemical Name |
N-(5-cyclobutyl-1H-pyrazol-3-yl)-2-naphthalen-2-ylacetamide
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| Synonyms |
CDK5 inhibitor 20223; CDK5 inhibitor 20 223
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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 : ~100 mg/mL (~327.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (16.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2747 mL | 16.3736 mL | 32.7472 mL | |
| 5 mM | 0.6549 mL | 3.2747 mL | 6.5494 mL | |
| 10 mM | 0.3275 mL | 1.6374 mL | 3.2747 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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