货号	规格	价格	上海	北京	珠海	重庆	武汉
T24428-5mg买3赠1	99.50%	￥1000.00 T24428-5mg ￥1000.00 现货（买3赠1）	3 3	-	-	-	-
T24428-10mg买3赠1	99.50%	￥1500.00 T24428-10mg ￥1500.00 现货（买3赠1）	5 5	-	-	-	-
T24428-25mg买3赠1	99.50%	￥2800.00 T24428-25mg ￥2800.00 现货（买3赠1）	5 5	-	-	-	-
T24428-100mg	99.50%	￥6500.00 T24428-100mg ￥6500.00 现货	3 3	-	-	-	-

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产品描述：

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。

靶点：

cdk2-cyclin A：7 μM (IC50)；cdk2-cyclin E：7 μM (IC50)

体外研究：

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.

体内研究：

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.

参考文献：

1. Vesely, J., Havlicek, J., Strnad, M., et al. Inhibition of cyclin-dependent kinases by purine analogues. European Journal of Biochemistry 224, 771-786 (1994).

2. Abraham, R.T., Acquarone, M., Andersen, A., et al. Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. Biology of the Cell 83(2), 105-120 (1995).

3. Hajdúch M, et al. Induction of apoptosis and regression of spontaneous dog melanoma following in vivo application of synthetic cyclin-dependent kinase inhibitor olomoucine. Anticancer Drugs. 1997 Nov. 8(10):1007-13.

4. Raynaud FI, et al. Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis. Mol Cancer Ther. 2004 Mar. 3(3):353-62.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.352 ml	16.759 ml	33.519 ml
5 mM	0.67 ml	3.352 ml	6.704 ml
10 mM	0.335 ml	1.676 ml	3.352 ml
50 mM	0.067 ml	0.335 ml	0.67 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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