Network Version
MLN8054 Data Sheet
| Product Name: | MLN8054 |
 |
|---|---|---|
| CAS No.: | 869363-13-3 | |
| Cat. No.: | HY-10180 | |
| MWt: | 476.86 | |
| Formula: | C25H15ClF2N4O2 | |
| Purity : | >98% | |
| Solubility: | H<sub>2</sub>O : < 0.1 mg/mL;DMSO : 30 mg/mL (ultrasonic;warming) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM. IC50 & Target: IC50: 4 nM (Aurora A), 172 nM (Aurora B)[1] In Vitro: MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase. MLN8054 is >40-fold more selective for Aurora A compared with the family member Aurora B. MLN8054 selectively inhibits Aurora A over Aurora B in cultured human tumor cells. MLN8054 treatment results in G2/M accumulation and spindle defects and inhibits proliferation in multiple cultured human tumor cells lines. MLN8054 effectively inhibits the growth of cells from diverse tissue origins with IC50 values ranging from 0.11 to 1.43 μM[1]. Treatment of human tumor cells grown in culture with MLN8054 shows a number of morphologic and biochemical changes associated with senescence[2]. In Vivo: In the HCT-116 tumor-bearing mice, MLN8054 treatment inhibits tumor growth dose dependently. MLN8054 is generally well tolerated. MLN8054 also inhibits the growth of the PC-3 tumor xenograft in nude mice. MLN8054 Treatment Results in Inhibition of Aurora A, Accumulation of Mitotic Cells, and Apoptosis in vivo[1]. MLN8054 selectively inhibits Aurora A kinase activity when dosed at 30 mg/kg. At this dose in HCT116 tumor tissue, MLN8054 has been shown to inhibit Aurora A autophosphorylation, and induce an increase in the Aurora B substrate, pHisH3[2]. | ||
1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Web:www.medchemexpress.com