PHA-680632Aurora kinase inhibitor,novel and potent CAS# 398493-79-3 |
Quality Control & MSDS
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| Cas No. | 398493-79-3 | SDF | Download SDF |
| PubChem ID | 11249084 | Appearance | Powder |
| Formula | C28H35N7O2 | M.Wt | 501.62 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 30 mg/mL (59.81 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-(2,6-diethylphenyl)-3-[[4-(4-methylpiperazin-1-yl)benzoyl]amino]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazole-5-carboxamide | ||
| SMILES | CCC1=C(C(=CC=C1)CC)NC(=O)N2CC3=C(C2)NN=C3NC(=O)C4=CC=C(C=C4)N5CCN(CC5)C | ||
| Standard InChIKey | OBWNXGOQPLDDPS-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C28H35N7O2/c1-4-19-7-6-8-20(5-2)25(19)29-28(37)35-17-23-24(18-35)31-32-26(23)30-27(36)21-9-11-22(12-10-21)34-15-13-33(3)14-16-34/h6-12H,4-5,13-18H2,1-3H3,(H,29,37)(H2,30,31,32,36) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PHA-680632 is a potent inhibitor of Aurora kinase with IC50 values of 27 nM, 135 nM and 120 nM for Aurora A, Aurora B and Aurora C, respectively. | |||||
| Targets | Aurora A | Aurora B | Aurora C | |||
| IC50 | 27 nM | 135 nM | 120 nM | |||
PHA-680632 Dilution Calculator
PHA-680632 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9935 mL | 9.9677 mL | 19.9354 mL | 39.8708 mL | 49.8385 mL |
| 5 mM | 0.3987 mL | 1.9935 mL | 3.9871 mL | 7.9742 mL | 9.9677 mL |
| 10 mM | 0.1994 mL | 0.9968 mL | 1.9935 mL | 3.9871 mL | 4.9839 mL |
| 50 mM | 0.0399 mL | 0.1994 mL | 0.3987 mL | 0.7974 mL | 0.9968 mL |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.3987 mL | 0.4984 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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PHA-680632 is a novel and potent inhibitor of Aurora kinases, a small family of serine/threonine kinases regulating mitosis in chromosome segregation and cell division, that inhibits the activity of all three Aurora kinases with 50% inhibition concentration IC50 values of 27 nM, 135 nM and 120 nM for Aurora A, B and C kinases respectively. PHA-680632 also cross-reacts with other kinases, including FGFR1, FLT3, LCK, PLK1, STLK2, VEGFR2 and VEGFR3, to a lesser extent and exhibits much higher IC50 values (390 to 5500 nM) compared to Aurora kinases. Moreover, PHA-680632 potently inhibits proliferation in a wide range of cancer cell types, including HCT116, A2780, HL60 and Hela cells, with IC50 values ranging from 0.06 to 7.15 μM.
Reference
Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9.
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PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity.[Pubmed:16818708]
Clin Cancer Res. 2006 Jul 1;12(13):4080-9.
PURPOSE: Aurora kinases play critical roles during mitosis in chromosome segregation and cell division. The aim of this study was to determine the preclinical profile of a novel, highly selective Aurora kinase inhibitor, PHA-680632, as a candidate for anticancer therapy. EXPERIMENTAL DESIGN: The activity of PHA-680632 was assayed in a biochemical ATP competitive kinase assay. A wide panel of cell lines was evaluated for antiproliferative activity. Cell cycle analysis. Immunohistochemistry, Western blotting, and Array Scan were used to follow mechanism of action and biomarker modulation. Specific knockdown of the targets by small interfering RNA was followed to validate the observed phenotypes. Efficacy was determined in different xenograft models and in a transgenic animal model of breast cancer. RESULTS: PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor growth inhibition in different animal tumor models at well-tolerated doses. The mechanism of action of PHA-680632 is in agreement with inhibition of Aurora kinases. Histone H3 phosphorylation in Ser10 is mediated by Aurora B kinase, and our kinetic studies on its inhibition by PHA-680632 in vitro and in vivo show that phosphorylation of histone H3 is a good biomarker to follow activity of PHA-680632. CONCLUSIONS: PHA-680632 is the first representative of a new class of Aurora inhibitors with a high potential for further development as an anticancer therapeutic. On treatment, different cell lines respond differentially, suggesting the absence of critical cell cycle checkpoints that could be the basis for a favorable therapeutic window.
