Phthalazinone pyrazole |
カタログ番号GC13668
One-Click Copy Product Info
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フタラジノン ピラゾールは、0.031 μM の IC50 を持つオーロラ A キナーゼの強力で選択的な経口活性阻害剤です。フタラジノンピラゾールは、有糸分裂を停止させ、その後、増殖細胞のアポトーシスを介して腫瘍の成長を阻害します。フタラジノン ピラゾールは、ヒト胚性幹細胞からの肝細胞様細胞 (HLC) の分化中の上皮間葉転換 (EMT) を抑制します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 880487-62-7
Sample solution is provided at 25 µL, 10mM.
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Phthalazinone pyrazole is potent, selective, and orally bioavailable inhibitor of Aurora-A kinase [1]. The Aurora protein kinase family consists of Aurora-A, -B and –C. The Aurora kinases are important group of enzymes involved in controlling several aspects of cell division in mammalian cells. Dysfunction of these kinases has been associated with a failure to maintain a stable chromosome content, a state that can contribute to tumourigenesis. Aurora-A is overexpressed in a variety of tumor types and displays oncogenic activity [2].
In vitro: Phthalazinone pyrazole potently inhibited the activity of Aurora A kinase with an IC50 of 31 nM. It showed no inhibitory effect on Aurora B kinase at doses up to 100 μM. Phthalazinone pyrazole inhibited the proliferation of HCT116, Colo205, and MCF-7 cells with IC50 values of 7.8, 2.9, and 1.6 μM, respectively [1].
References:
[1] Prime M E, Courtney S M, Brookfield F A, et al. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase[J]. Journal of medicinal chemistry, 2010, 54(1): 312-319.
[2] Vader G, Lens S M A. The Aurora kinase family in cell division and cancer[J]. Biochimica et Biophysica Acta (BBA)-Reviews on Cancer, 2008, 1786(1): 60-72.
| Cas No. | 880487-62-7 | SDF | |
| Chemical Name | 4-[(5-methyl-1H-pyrazol-3-yl)amino]-2H-phenyl-1-phthalazinone | ||
| Canonical SMILES | O=C1C2=C(C=CC=C2)C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4 | ||
| Formula | C18H15N5O | M.Wt | 317.4 |
| 溶解度 | ≤0.15mg/ml in DMSO;0.25mg/ml in dimethyl formamide | Storage | Store at -20°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 | 3.1506 mL | 15.753 mL | 31.506 mL |
| 5 mM | 630.1 μL | 3.1506 mL | 6.3012 mL |
| 10 mM | 315.1 μL | 1.5753 mL | 3.1506 mL |
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μL
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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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)