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- Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Kimura M, .et al. Aurora A regulates the architecture of the Golgi apparatus, Exp Cell Res, 2018, Jun 1;367(1):73-80 PMID: 29571950
- Jing Wang, .et al. The Aurora-A-Twist1 axis promotes highly aggressive phenotypes in pancreatic carcinoma, J Cell Sci, 2017, Mar 15; 130(6): 1078-1093 PMID: 28167680
- Lessing D, .et al. A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation, Proc Natl Acad Sci U S A, 2016, Dec 13;113(50):14366-14371 PMID: 28182563
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
Biological Activity
MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3..
| In vitro (25°C) | DMSO | 23 mg/mL (44.32 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 5%DMSO+30% PEG300+5%Tween-80+ddH2O | 5 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 19.27 mL | 96.36 mL | 192.72 mL |
| 0.5 mM | 3.85 mL | 19.27 mL | 38.54 mL |
| 1 mM | 1.93 mL | 9.64 mL | 19.27 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.85 mL |
*The above data is based on the productmolecular weight 518.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10004 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1028486-01-2 |
| Formula | C27H20ClFN4O4 |
| M. Wt | 518.9 |
| Purity | >98% |
| SMILES | COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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