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Olomoucine

cdk抑制剂，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)。

目录号: PC10010 纯度: ≥98%

CAS No. :101622-51-9

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中文名称

Olomoucine

中文别名

2-(2'-羟基乙基氨基)-9-甲基-6-(苄基氨基)嘌呤;2-(2´-羟基乙基氨基)-9-甲基-6-(苄基氨基)嘌呤;2-(2''-羟基乙基氨基)-9-甲基-6-(苄基氨基)嘌呤;2-(2-羟基乙基氨基)-9-甲基-6-(苄基氨基)嘌呤;2-(羟乙氨基)-6-苄氨基-9-甲基嘌呤;奥罗莫星

英文名称

Olomoucine

英文别名

Ethanol,2-[[9-methyl-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-;Olomoucine;2-[[6-(benzylamino)-9-methylpurin-2-yl]amino]ethanol;OLO;Olomoucine,high purity;2-(Hydroxyethylamino)-6-benzylamino-9-methylpurine;6-(Benzylamino)-2-(2-hydroxyethylamino)-9-methylpurine;NSC 666096;N2-[(2-HYDROXYETHYL)]-N6-BENZYLADENINE;6-BENYLAMINO-2-(2-HYDROXYETHYLAMINO)-9-METHYLPURINE;6-BENZYLAMINO-2-(2-HYDROXYETHYLAMINO)-9-METHYLPURINE;2-(2-HYDROXYETHYLAMINO)-6-BENZYLAMINO-9-METHYLPURINE;Olomoucine,highpurity;OLOMOUCINE SYNTHETIC >95%;Olomoucine,98%,high purity

Cas No.

101622-51-9

分子式

C₁₅H₁₈N₆O

分子量

298.34

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.

性状

Solid

IC50 & Target[1][2]

cdk2-cyclin A

7 μM (IC₅₀)

cdk2-cyclin E

7 μM (IC₅₀)

cdk5-p35

25 μM (IC₅₀)

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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	C_max (nM)	Cl_obs (l/h)	V_ss(obs) (l)	MRT_last (h)	AUC_inf(obs) (nMh)	t_1/2 (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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Dog with spontaneous melanoma (oral and maxillofacial tumors)
Dosage:	8 mg/kg
Administration:	Intravenous injection; once daily; for 7 days
Result:	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).

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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). [Information]

[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). [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 66.67 mg/mL (223.47 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3519 mL	16.7594 mL	33.5188 mL
5 mM	0.6704 mL	3.3519 mL	6.7038 mL
10 mM	0.3352 mL	1.6759 mL	3.3519 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (8.38 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.38 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.38 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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