Alisertib (MLN8237), Aurora A inhibitor (TBI4124)

Description

Product Details

Formal Name: 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid

Alternate Names: MLN8237

Molecular Formula: C₂₇H₂₀ClFN₄O₄

Formula Weight: 518.90

CAS Number: 1028486-01-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 5 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Aurora A inhibitor

Functions

Highly potent, ATP-competitive inhibitor selective for Aurora A kinase (Ki = 0.3 nM; IC50 = 6.7 nM) over Aurora B (IC50 = 1.5 µM); does not inhibit a large panel of other kinases. Also exhibits off-target binding of GABAA (IC50 = 0.49 µM), but no effects attributable to this binding were observed in rats. Disrupts the Aurora A / Myc complex, resulting in Myc degradation in Myc-amplified neuroblastomas. Inhibits tumor cell growth in vitro and in vivo, causing apoptosis and autophagy, disrupted mitosis, and increased chromosome alignment abnormalities.

Application Procedures

First dissolved in DMSO (up to 5 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.