MLN8054 - CAS 869363-13-3
Catalog number: 869363-13-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Targets:
Aurora Kinase
Description:
MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers.
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Current Developer:
Millennium Pharmaceuticals Inc.
1.MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
Sells TB1, Chau R1, Ecsedy JA1, Gershman RE1, Hoar K1, Huck J1, Janowick DA1, Kadambi VJ1, LeRoy PJ1, Stirling M1, Stroud SG1, Vos TJ1, Weatherhead GS1, Wysong DR1, Zhang M1, Balani SK1, Bolen JB1, Manfredi MG1, Claiborne CF1. ACS Med Chem Lett. 2015 Apr 22;6(6):630-4. doi: 10.1021/ml500409n. eCollection 2015.
The Aurora kinases are essential for cell mitosis, and the dysregulation of Aurora A and B have been linked to the etiology of human cancers. Investigational agents MLN8054 (8) and alisertib (MLN8237, 10) have been identified as high affinity, selective, orally bioavailable inhibitors of Aurora A that have advanced into human clinical trials. Alisertib (10) is currently being evaluated in multiple Phase II and III clinical trials in hematological malignancies and solid tumors.
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CAS 869363-13-3 MLN8054

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