Olomoucine,101622-51-9

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Olomoucine

CAS No. : 101622-51-9

MCE 国际站：Olomoucine

产品活性：Olomoucine 是 ATP 竞争性的 CDKs 的抑制剂。Olomoucine 是一种嘌呤 (HY-34431) 衍生物，可抑制 CDC2/cyclin B, Cdk2/cyclin a, Cdk2/cyclin E (IC₅₀=7 µM)，CDK/p35 激酶 (IC₅₀=3 µM) 和 ERK1/p44 MAPK 激酶的活性 (IC₅₀=25 µM)。Olomoucine 也具有调节细胞周期和抗黑色素肿瘤的能力。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

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.
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.

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

Administration	Cmax (nM)	Clobs (l/h)	Vss(obs) (l)	MRTlast (h)	AUCinf(obs) (nM.h)	t1/2 (h)
cassettle	9208 (0.9)	1.10	0.67 (2.8)/td>	0.56	3030	1.03 (0.7)
single	7194 (0.6)	1.18	0.52 (2.1)/td>	0.40	2831	0.98 (0.7)

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

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