| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Pim-1 kinase inhibitor 8 targets Pim-1 kinase, a serine/threonine kinase that belongs to the Pim (Proviral Integration site for Moloney murine leukemia virus) family. Pim-1 is a proto-oncogene that is overexpressed in various hematological malignancies and solid tumors, including prostate cancer, breast cancer, and hepatocellular carcinoma. Pim-1 phosphorylates and regulates the activity of multiple substrates involved in cell cycle progression, apoptosis, and protein synthesis. By inhibiting Pim-1 kinase activity, this compound suppresses downstream signaling pathways that promote cancer cell proliferation and survival.
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| ln Vitro |
Pim-1 kinase inhibitor 8 shows potent in vitro activity against Pim-1 kinase with an IC50 of 14.3 nM. The compound demonstrates potent cytotoxicity against MCF-7 breast cancer cells with an IC50 of 0.5 μM and against HepG2 hepatocellular carcinoma cells with an IC50 of 5.27 μM. The compound also effectively inhibits cell migration, suggesting potential activity against cancer metastasis. The selectivity of Pim-1 kinase inhibitor 8 for Pim-1 over other kinases has not been detailed in the available literature.
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| ln Vivo |
In vivo activity of Pim-1 kinase inhibitor 8 has been suggested based on its potent in vitro activity and anticancer properties. As a Pim-1 kinase inhibitor, the compound has the potential to suppress tumor growth in xenograft models of Pim-1-dependent cancers. However, detailed in vivo efficacy data have not been extensively reported in the available literature. The compound is a candidate compound for breast cancer research.
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| Enzyme Assay |
Non-cell-based kinase assays for Pim-1 kinase inhibitor 8 typically involve measuring the inhibition of recombinant Pim-1 kinase activity using a radioactive or fluorescence-based assay. A standard protocol includes: incubating purified Pim-1 kinase with a peptide substrate (such as a biotinylated Pim-1 substrate peptide) and ATP in kinase buffer (pH 7.4). Pim-1 kinase inhibitor 8 is added at various concentrations (typically 0.001–100 μM), and the phosphorylation of the substrate is measured using a scintillation proximity assay or time-resolved fluorescence resonance energy transfer (TR-FRET). IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for Pim-1 kinase inhibitor 8 typically involve cancer cell lines that are dependent on Pim-1 activity, such as MCF-7 breast cancer cells or HepG2 hepatocellular carcinoma cells. A representative protocol includes: culturing cells in appropriate medium, treating with Pim-1 kinase inhibitor 8 at various concentrations (0.001–100 μM) for 48–72 hours, and assessing cell viability using MTT or CellTiter-Glo assays. To confirm on-target activity, Pim-1 kinase activity and phosphorylation of downstream substrates (e.g., p-BAD) are measured by Western blot. Cell migration is assessed using scratch wound healing or Transwell assays.
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| Animal Protocol |
In vivo animal studies with Pim-1 kinase inhibitor 8 have not been extensively reported in the available literature. If conducted, a typical protocol would involve xenograft mouse models of breast cancer or hepatocellular carcinoma, with administration of the compound via oral gavage or intraperitoneal injection at doses determined from pharmacokinetic studies. Tumor growth and body weight would be monitored, and tumors would be harvested for analysis of Pim-1 kinase activity and downstream signaling.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Pim-1 kinase inhibitor 8 have not been extensively reported in the available literature. As a small molecule with a molecular weight of 275.30 g/mol, it is expected to have reasonable oral bioavailability. The compound is typically stored as a powder at -20°C. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
As a research compound, Pim-1 kinase inhibitor 8 is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening in normal cell lines, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity.
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| References | |
| Additional Infomation |
Pim-1 kinase inhibitor 8 (Compound 12, CAS 916038-47-6) is a potent Pim-1 kinase inhibitor with an IC50 of 14.3 nM. The compound demonstrates potent cytotoxicity against MCF-7 breast cancer cells and HepG2 hepatocellular carcinoma cells and effectively inhibits cell migration. Pim-1 kinase is a validated target in cancer, particularly in hematological malignancies and solid tumors, and this compound provides a valuable research tool for investigating the therapeutic potential of Pim-1 inhibition. The compound is a candidate for breast cancer research.
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| Molecular Formula |
C14H17N3O3
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|---|---|
| Molecular Weight |
275.303083181381
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| Exact Mass |
275.126
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| CAS # |
916038-47-6
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| PubChem CID |
17186393
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| Appearance |
White to off-white solid powder
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
386
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=NC(=C1C#N)OCC(=O)N2CCOCC2)C
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| InChi Key |
XARGLDJCVPQGEH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17N3O3/c1-10-7-11(2)16-14(12(10)8-15)20-9-13(18)17-3-5-19-6-4-17/h7H,3-6,9H2,1-2H3
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| Chemical Name |
4,6-dimethyl-2-(2-morpholin-4-yl-2-oxoethoxy)pyridine-3-carbonitrile
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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 :~125 mg/mL (~454.05 mM; with sonication)
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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 | 3.6324 mL | 18.1620 mL | 36.3240 mL | |
| 5 mM | 0.7265 mL | 3.6324 mL | 7.2648 mL | |
| 10 mM | 0.3632 mL | 1.8162 mL | 3.6324 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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