TCS PIM-1 1 (Synonyms: SC 204330) |
Catalog No.GC17178 |
A Pim-1 kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 491871-58-0
Sample solution is provided at 25 µL, 10mM.
TCS PIM-1 1 is a selective inhibitor of Pim-1 with IC50 value of 50 nM [1].
Pim-1 is a proto-oncogene serine/threonine-protein kinase and plays an important role in cell cycle progression, apoptosis, transcriptional activation and more general signal transduction pathways. It has been shown that Pim-1 over-expression is correlated with a variety of human cancers [2].
TCS PIM-1 1 is a potent Pim-1 inhibitor and has a better selectivity to Pim-1 than to Pim-2. It was revealed that TCS PIM-1 1 was the most potent inhibitor of Pim-1 by outlining the crystal structure and it was also shown that TCS PIM-1 1 had better inhibitory activity to Pim-1 compared with Pim-2 [1].
References:
[1]. Cheney, I.W., et al., Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett, 2007. 17(6): p. 1679-83.
[2]. Cen, B., et al., The Pim-1 protein kinase is an important regulator of MET receptor tyrosine kinase levels and signaling. Mol Cell Biol, 2014. 34(13): p. 2517-32.
Cas No. | 491871-58-0 | SDF | |
Synonymes | SC 204330 | ||
Chemical Name | 6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile | ||
Canonical SMILES | O=C1C(C#N)=C(C2=CC=CC=C2)C=C(C3=C(O)C=CC(Br)=C3)N1 | ||
Formula | C18H11BrN2O2 | M.Wt | 367.2 |
Solubility | ≥ 12.8mg/mL in DMSO | Storage | Store at 4°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.7233 mL | 13.6166 mL | 27.2331 mL |
5 mM | 0.5447 mL | 2.7233 mL | 5.4466 mL |
10 mM | 0.2723 mL | 1.3617 mL | 2.7233 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
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