2241914-86-1

2241914-86-1 structure
2241914-86-1 structure
  • Name: Aurora Kinases-IN-2
  • Chemical Name: Aurora Kinases-IN-2
  • CAS Number: 2241914-86-1
  • Molecular Formula: C22H18ClN5O3
  • Molecular Weight: 435.86
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Aurora Kinase
  • Create Date: 2022-08-31 19:10:06
  • Modify Date: 2024-01-16 09:25:10
  • Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research[1].

Name Aurora Kinases-IN-2
Description Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research[1].
Related Catalog
Target

Aurora A:90 nM (IC50)

Aurora B:152 nM (IC50)

In Vitro Aurora Kinases-IN-2 (compound 12Aj) (72 hours) has antiproliferative activity with IC50 values of 11.5 μM, 1.34 μM, 7.30 μM and 1.64 μM for U87, HeLa, HepG2 and LoVo tumor cell lines, respectively[1]. Aurora Kinases-IN-2 (compound 12Aj) (0-10 μM; 24 hours) inhibits Aurora A and Aurora B in HeLa cells[1]. Aurora Kinases-IN-2 (compound 12Aj) (0-10 μM; 24 hours; HeLa cells) results in G2/M accumulation by regulating the expression of Cyclin B1 and cdc2[1]. Aurora Kinases-IN-2 (compound 12Aj) (0-10 μM; 24 hours) blocks phosphorylation of Aurora kinases in HeLa cells[1]. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0, 1, 5 and 10 μM Incubation Time: 24 hours Result: Decreased the expression level of Aurora A and B, as well as reduced phosphorylation of Aurora A on Thr288 (p-Thr288) and Aurora B on Thr232 (p-Thr232) in a dose-dependent manner.
References

[1]. Bo YX, et, al. Synthesis, biological evaluation and molecular modeling study of 2-amino-3,5-disubstituted-pyrazines as Aurora kinases inhibitors. Bioorg Med Chem. 2020 Mar 1;28(5):115351.

Molecular Formula C22H18ClN5O3
Molecular Weight 435.86