Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM)[2]. Olomoucine regulates cell cycle and shows anti-melanin tumor activity.IC50 & Target: Target: CDK (cyclin-dependent kinases)In Vitro: Olomoucine inhibits CDK2 and CDC2 kinases with IC50 of 7 μM (CDC2/cyclin B), 7 μM (CDK2/cyclin A), 7 μM (CDK2/cyclin E), 3 Μm (CDK5/p35), and 25μM (ERK1/p44 MAPK), respectively.
Olomoucine (0, 5, 10, 15, and 25 μM) is a competitive inhibitor for ATP and as a non-competitive inhibitor for histone H.
Olomoucine (0-1000 μM) inhibits DNA synthesis in interleukin-2-stimulated T lymphocytes (CTLL-2 cells) and triggers a Gl arrest similar to interleukin-2 deprivation[2].
Olomoucine (0-100 μM) inhibits Gl/S transition of non-small cell lung cancer cell line MB65 cells[2].
Olomoucine (0-150 μM) inhibits prophase/metaphase transition of Rdditapes oocytes[2].
Olomoucine inhibits tumor cells survival with IC50s of 32.35 μM (dog melanoma), 42.15 μM (mouse B16 melanoma), 82.30 μM (human melanoma), respectively.In Vivo: Olomoucine (8 mg/kg; i.v.; once daily; 7 d) induces apoptosis in tumor cells on the 3rd day after treatment without side effects.
Cassette dosing was found to overestimate the AUC while underestimating the Cmax compared with single dosing administration.

Cassette dosing pharmacokinetics for olomoucine

Note: Single agents dosing=50 mg/kg, cassette dosing=16.66 mg/kg.