Olomoucine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的 ATP 竞争性 CDK 抑制剂，对 Cdc2/cyclin B、Cdk2/cyclin A、Cdk2/cyclin E 和 Cdk/p35 激酶的 IC50 为 7, 7, 7, 3 uM；还抑制 ERK1/MAP 激酶 (IC50=25 uM)。

A potent, ATP-competetive CDKs inhibitor with IC50 of 7, 7, 7, 3 uM for Cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk/p35 kinase; also inhibits ERK1/MAP kinase (IC50=25 uM); inhibits the starfish oocyte G2/M transition in vivo.

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.Olomoucine (0-100 μM) inhibits Gl/S transition of non-small cell lung cancer cell line MB65 cells.Olomoucine (0-150 μM) inhibits prophase/metaphase transition of Rdditapes oocytes.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.

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.Animal Model:Dog with spontaneous melanoma (oral and maxillofacial tumors)Dosage:8 mg/kgAdministration:Intravenous injection; once daily; for 7 daysResult:Induced programmed cell death of cancer cells and resulted in rapid eradication of at least 68% of the tumor cells.Animal Model:Female Balb C? mice (6 weeks of age; weight of 20 g (±1.2 g))Dosage:50 mg/kg (single agent) or 16.6 mg/kg combinded with purines (cassette)Administration:Intravenous injection (tail vein); samples taken at 0.25, 0.5, 1, 2, 4, 6, and 24 h post-dosing Result:Resulted faster plasma concentration decreasing with 50 mg/kg (as single agent) than 16.6 mg/kg (as cassette).

Olomoucine

Angiogenesis

CDK

CDK

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101622-51-9

298.35

C15H18N6O

>98% (HPLC)

In Vitro:?DMSO : 66.67 mg/mL (223.47 mM)

CN1C=NC2=C(NCC3=CC=CC=C3)N=C(NCCO)N=C12

2-(2-Hydroxyethylamino)-6- benzylamino-9-methylpurine

(-20℃)

With Ice Pack

≥ 2 years