MLN-8237 is a second-generation, selective Aurora A kinase (AAK) inhibitor with an IC50 of 1 nM. MLN8237 shows 200-fold more selective activity against Aurora-A than related kinase Aurora-B. Inhibition of AAK by MLN-8237 induces cytotoxicity and cell arrest. Several completed as well as actively on-going phase I/II clinical trials evaluate MLN-8237 in advanced solid tumor as well as advanced hematological malignancies.
Technical information:
| Chemical Formula: | C27H2OClFN4O4 | |
| CAS #: | 1028486-01-2 | |
| Molecular Weight: | 518.92 | |
| Purity: | >98% | |
| Appearance: | White solid | |
| Chemical Name: | 4-((9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido[4,5-e]azepin-2-yl)amino)-2-methoxybenzoic acid | |
| Solubility: | Up to 50 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Gorgun G et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma. Blood. 2010; 115(25): 5202–5213. |
| 2. | Manfredi MG et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays. Clin Cancer Res. 2011; 17(24):7614-24. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
