Olomoucine 是 CDK2/cyclin A、Cdc2/CyclinB、CDK2/CyclinE、CDK5/p35 和 ERK1/p44 MAP 激酶的 ATP 竞争性抑制剂，IC50 分别为 7、7、7、3 和 25 μM。 Olomoucine 调节细胞周期并表现出抗黑色素肿瘤活性。

Olomoucine is an ATP competitive inhibitor of Cdk2/cyclin A, Cdc2/CyclinB, CDK2/CyclinE, CDK5/p35, and ERK1/p44 MAP kinase with IC50s of 7, 7, 7, 3 and 25 μM, respectively. Olomoucine regulates cell cycle and exhibits anti-melanin tumor activities.

In Rdditapes oocytes, Olomoucine (0-150 μM) inhibits prophase/metaphase transition. In CTLL-2 cells, Olomoucine (0-1000 μM) inhibits DNA synthesis and triggers a Gl arrest similar to interleukin-2 deprivation. In NSCLC MB65 cells, Olomoucine (0-100 μM) inhibits Gl/S transition[1]. Olomoucine inhibits tumor cell survival with IC50s of 32.35, 42.15, and 82.30 μM for dog, mouse B16, and human melanoma, respectively[4].

In female Balb C– mice, Olomoucine results faster plasma concentration decreasing with 50 mg/kg (as single agent) than 16.6 mg/kg (as cassette)[3]. In dog with spontaneous melanoma, Olomoucine (8 mg/kg; i.v.) induces programmed cell death of cancer cells and results in rapid eradication of at least 68% of the tumor cells without side effects[4].

101622-51-9

C15H18N6O

298.34

DMSO:95 mg/mL (318.43 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years