869363-13-3 Usage
Uses
MLN 8054 is an Aurora kinase inhibitor, used to treat patients with advanced solid tumors.
Biological Activity
mln8054 is a potent of aurora a kinase (aak) inhibitor consisting of a benzazepine core scaffold with a fused amino pyrimidine and an aryl carboxylic acid which represents an unprecedented kinase inhibitor framework. the inhibition of mln8054 towards aak is atp-competitive, reversible and selective with an ic50 value of 4nm, which is more than 40-fold and 100-fold selective comparing to aurora b kinase (ic50 = 175 nm) and a range of other kinases respectively. mln8054 exerts antitumor activity against human tumor xenografts through aak inhibition, which results in deactivation of pt288, spindle defects, accumulation of g2/m, and apoptosis-induced cell death in tumor cells.mark g. manfredi, jeffery a. ecsedy, kristan a. meetze, suresh k. balani, olga burenkova. wei chen, katherine m. galvin, kara m. hoar, jessica j. huck, patrick j. leroy, emily t. ray, todd b. sells, bradley stringer, stephen g. stroud, tricia j. vos, gabriel s. weatherhead, deborah r. wysong, mengkun zhang, joseph b. bolen, and christopher f. claiborne. antitumor activity of mln8054, an orally active small-molecule inhibitor of aurora a kinase. pnas 2007; 104(10): 4106-4111
Check Digit Verification of cas no
The CAS Registry Mumber 869363-13-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,9,3,6 and 3 respectively; the second part has 2 digits, 1 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 869363-13:
(8*8)+(7*6)+(6*9)+(5*3)+(4*6)+(3*3)+(2*1)+(1*3)=213
213 % 10 = 3
So 869363-13-3 is a valid CAS Registry Number.
InChI:InChI=1/C25H15ClF2N4O2/c26-15-6-9-17-18(10-15)23(21-19(27)2-1-3-20(21)28)29-11-14-12-30-25(32-22(14)17)31-16-7-4-13(5-8-16)24(33)34/h1-10,12H,11H2,(H,33,34)(H,30,31,32)
869363-13-3Relevant articles and documents
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors
Sells, Todd B.,Chau, Ryan,Ecsedy, Jeffrey A.,Gershman, Rachel E.,Hoar, Kara,Huck, Jessica,Janowick, David A.,Kadambi, Vivek J.,Leroy, Patrick J.,Stirling, Matthew,Stroud, Stephen G.,Vos, Tricia J.,Weatherhead, Gabriel S.,Wysong, Deborah R.,Zhang, Mengkun,Balani, Suresh K.,Bolen, Joseph B.,Manfredi, Mark G.,Claiborne, Christopher F.
, p. 630 - 634 (2015/06/30)
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,
Compounds and methods for inhibiting mitotic progression
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Page/Page column 145, (2008/06/13)
This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treat
