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Alisertib | Potent and selective inhibitor of Aurora A / Destabilizes Myc

Alisertib (MLN8237, 1028486-01-2) is a highly selective and potent (IC50 = 1 nM) cell permeable inhibitor of Aurora A with off-target binding at GABAA (IC50 = 490 nM).1 It disrupts the Aurora A-Myc complex leading to Myc degradation2 in Myc amplified neuroblastomas3 and p53-mutant human hepatocellular carcinoma cell4. Alisertib has been found to induce apoptosis and autophagy in breast cancer5 and melanoma6 cells via suppression of activation of the p38 MAPK pathway.

References/Citations

1) Sells et al. (2015), MLN8054 and Alisertib (MLN8237):Discovery of Selective Oral Aurora A Inhibitors; ACS Med. Chem. Lett. 6 630
2) Richards et al. (2016), Structural basis of N-Myc binding by Aurora-A and its destabilization by kinase inhibitors; Proc. Natl. Acad. Sci. USA 113 13726
3) Brockmann et al. (2013), Small molecule inhibitors of aurora-a induce proteasomal degradation of N-myc in childhood neuroblastoma; Cancer Cell 24 75
4) Dauch et al. (2016), A MYC-aurora kinase A protein complex represents an actionable drug target in p53-altered liver cancer; Nat. Med. 22 744
5) Li et al. (2015), The investigational Aurora kinase A inhibitor alisertib (MLN8237) induces cell cycle G2/M arrest, apoptosis, and autophagy via p38 MAPK and Akt/mTOR signaling pathways in human breast cancer cells; Drug Des. Devel. Ther. 16 1627
6) Shang et al. (2017), Alisertib promotes apoptosis and autophagy in melanoma through p38 MAPK-mediated aurora a signaling; Oncotarget 8 107076

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Catalog#  10-4124-0005

$60.00
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CAS:
1028486-01-2
Catalog Number:
10-4124
Activity:
Potent and selective inhibitor of Aurora A / Destabilizes Myc
Chemical 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 Weight:
518.27
Molecular Formula:
C27H20ClFN4O4
Solubility:
Soluble in DMSO (up to 5 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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