NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1/cyclinB, CDK2/cyclinA3, CDK1/CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.

CDK1-CyclinB:9.5 nM, DYRK1A:0.9 μM, PDK1:0.8 μM, CDK2-CyclinA3:5.4 nM, CDK4:1.6 μM

Treatment with NU6102 (0-30 μM; 1-24 hours) induces G2 arrest, inhibition of Rb phosphorylation, and cytotoxicity (LC50 2.6 μM for a 24-hour exposure) in SKUT-1B cells[3]. NU6102 inhibits cell growth and causes cell cycle phase arrest in human breast cancer cell lines, displaying G2/M arrest in asynchronously growing cell lines and G1/S arrest in cells released from serum starvation, and in Xenopus nuclei in a time-dependent manner[3]. Moreover, NU6102 selectively inhibits the growth of CDK2 WT (wild type) compared to KO MEFs (knockout mouse embryo fibroblasts) with a GI50 of 14 μM versus >30 μM[3].

The pharmacokinetics of NU6102 are determined in Balb/C mice following i.v. and i.p. administration. Due to the limited solubility of NU6102, 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. After i.v. administration, peak plasma levels of 12 μM NU6102 are observed 5 minutes post-administration, while the peak concentration achieved with the maximum administrable dose of NU6102 i.v. is 0.92 μM. The plasma half-life of NU6102 liberated following NU6301 administration is 42 minutes after i.p. and 10 minutes after i.v. administration[3].