NU6102

NU6102 is a potent CDK1 and CDK2 inhibitor with IC₅₀s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. NU6102 shows selectivity for CDK1/CDK2 over CDK4 (IC₅₀ of 1.6 μM), DYRK1A (IC₅₀ of 0.9 μM), PDK1 (IC₅₀ of 0.8 μM) and ROCKII (IC₅₀ of 0.6 μM)^[1][2]. In Vitro: NU6102 (0-30 μM; 1-24 hours; SKUT 1B cells) treatment induces a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LC₅₀ 2.6 μM for a 24 h exposure) in SKUT-1B cells^[3].
NU6102 inhibits cell growth and causes cell cycle phase arrest in human breast cancer cell lines, G2/M arrest in asynchronously growing cell lines and G1/S arrest in cells released from serum starvation, and in Xenopus nuclei in a timedependent manner^[3].
NU6102 selectively inhibits the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GI₅₀ of 14 μM versus >30 μM)^[3]. In Vivo: The pharmacokinetics of NU6102 is determined following i.v. and i.p. administration in Balb/C mice. The limited solubility of NU6102 meant the maximum administrable dose is 1 mg/kg i.v. and 10 mg/kg i.p. NU6102 is liberated following either i.p. or i.v. administration of NU6301, and following i.v. administration peak plasma levels of 12 μM NU6102 is observed 5 min post administration, whereas following administration of the maximum administrable dose of NU6102 i.v. the peak concentration achieved is 0.92 μM. The plasma half-life of NU6102 liberated following administration of NU6301 is 42 min following i.p. and 10 min following i.v. administration^[3].