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

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:
518.92
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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$60.00
25 mg$230.00

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

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:
518.92
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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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