JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC₅₀s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.

JNJ-7706621 shows antiproliferative activity against various human tumor cells with IC₅₀s of 284, 254, and 447 nM for HeLa, HCT116, and A375, respectively. JNJ-7706621 inhibits other centrosomal proteins such as TOG, Nek2, and TACC3 in early mitotic phase, but does not prevent localization of Aurora A to the spindle poles. Treatment of nocodazole-synchronized cells with JNJ-7706621 can override mitotic arrest by preventing spindle checkpoint signaling, resulting in failure of chromosome alignment and segregation. JNJ-7706621 shows inhibition of Aurora-A and Aurora-B but has no activity at the highest concentration tested on the Plk1 or Wee1 serine/threonine kinases. JNJ-7706621 also shows potent growth inhibition in vitro on all human cancer cell types with IC₅₀ values ranging from 112 to 514 nM. JNJ-7706621 suspensions inhibits cell viability of HeLa cells with IC₅₀s of 2.1 and 0.9 μg/mL at 24 and 48 h. The IC₅₀ of the JNJ-7706621-loaded nanoparticles are 35 and 2.7 μg/mL and the IC₅₀ of the JNJ-7706621-loaded micelles are 6.3 and 1.6 μg/mL^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-7706621 (100 and 125 mg/kg) is efficacious in a human tumor xenograft model under intermittent dosing regimens. JNJ-7706621 (100 mg/kg, i.p.) exhibits 95% tumor growth inhibition in A375 (human melanoma) tumor xenograft model. JNJ-7706621-loaded micelles inhibit tumor growth, and delay the tumor growth more efficiently than the control JNJ-7706621 suspension^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-7706621 (100 and 125 mg/kg) is efficacious in a human tumor xenograft model under intermittent dosing regimens. JNJ-7706621 (100 mg/kg, i.p.) exhibits 95% tumor growth inhibition in A375 (human melanoma) tumor xenograft model. JNJ-7706621-loaded micelles inhibit tumor growth, and delay the tumor growth more efficiently than the control JNJ-7706621 suspension^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Huang S, et al. Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6.  [Content Brief]

  . Matsuhashi A, et al. Growth suppression and mitotic defect induced by JNJ-7706621, an inhibitor of cyclin-dependent kinases and aurora kinases. Curr Cancer Drug Targets. 2012 Jul;12(6):625-39.  [Content Brief]

  . Emanuel S, et al. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 2005 Oct 1;65(19):9038-46.  [Content Brief]

  [4]. Danhier F, et al. Active and passive tumor targeting of a novel poorly soluble cyclin dependent kinase inhibitor, JNJ-7706621. Int J Pharm. 2010 Jun 15;392(1-2):20-8.  [Content Brief]