Alisertib (MLN8237) is a selective, small-molecule inhibitor of Aurora A kinase (AURKA), a serine/threonine kinase critical for mitotic entry, centrosome maturation, and spindle assembly. It exhibits potent in vitro activity with an IC₅₀ of approximately 1.2 nM against AURKA, while showing over 200-fold selectivity versus Aurora B and C kinases. In cellular assays, alisertib induces mitotic spindle abnormalities, leading to G2/M cell cycle arrest and subsequent apoptosis in cancer cells. Preclinical studies have demonstrated nanomolar antiproliferative activity in a broad range of tumor cell lines, including neuroblastoma, breast, colorectal, and hematologic malignancies, with in vivo tumor regression observed in xenograft models at doses of 10–30 mg/kg.
MedKoo Cat#: 573671
Name: Alisertib sodium
CAS#: 1028486-06-7 (sodium)
Chemical Formula: C27H19ClFN4NaO4
Exact Mass: 540.0977
Molecular Weight: 540.91
Elemental Analysis: C, 59.95; H, 3.54; Cl, 6.55; F, 3.51; N, 10.36; Na, 4.25; O, 11.83
The following data is based on the product molecular weight 540.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |