製品番号: HY-W011428

Olomoucine

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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.

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純度: 99.88%
CAS 番号: 101622-51-9
分子式: C₁₅H₁₈N₆O
分子量:298.34

保管条件:

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

Olomoucine 構造式

CAS 番号: 101622-51-9

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生物活性
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- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
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純度とドキュメンテーション
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製品説明

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)^[1]^[2]. Olomoucine regulates cell cycle and shows anti-melanin tumor activity^[3]^[4].

IC₅₀ & Target^[1]

cdk2-cyclin A

7 μM (IC₅₀)

cdk2-cyclin E

7 μM (IC₅₀)

cdk5-p35

25 μM (IC₅₀)

CDK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	16.6 μM Compound: Olomoucine	Growth inhibition of human A431 cells after 2 days by SRB assay Growth inhibition of human A431 cells after 2 days by SRB assay	[PMID: 22000924]
A549	IC₅₀	57 μg/mL Compound: Olomoucine	Inhibition of A549 cancer cell proliferation Inhibition of A549 cancer cell proliferation	[PMID: 10743948]
A549	IC₅₀	130 μM Compound: Olomoucine	Cytotoxicity against human A549 cells assessed as growth inhibition after 24 to 48 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as growth inhibition after 24 to 48 hrs by CCK8 assay	[PMID: 23933045]
B16-F10	IC₅₀	105 μM Compound: 5	Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay	[PMID: 22819191]
CCRF-CEM	IC₅₀	62 μM Compound: Olomoucine	In vitro cytotoxic effect on CEM cancer cell line In vitro cytotoxic effect on CEM cancer cell line	[PMID: 12392733]
COLO1	IC₅₀	87 μg/mL Compound: Olomoucine	Inhibition of Col1 cancer cell proliferation Inhibition of Col1 cancer cell proliferation	[PMID: 10743948]
G-361	IC₅₀	160 μM Compound: Olomoucine	In vitro cytotoxic effect on G361 cancer cell line In vitro cytotoxic effect on G361 cancer cell line	[PMID: 12392733]
G-361	IC₅₀	147 μM Compound: olomoucine	Antiproliferative activity against G361 cell line Antiproliferative activity against G361 cell line	[PMID: 17064068]
HCT-15	IC₅₀	62.5 μM Compound: Olomucine	Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay	[PMID: 20045224]
HeLa S3	GI₅₀	65 μM Compound: 1	Antiproliferative activity against human HeLaS3 cells by sulforhodamine B assay Antiproliferative activity against human HeLaS3 cells by sulforhodamine B assay	[PMID: 19846305]
HL-60	IC₅₀	50 μg/mL Compound: Olomoucine	Inhibition of HL60 cancer cell proliferation Inhibition of HL60 cancer cell proliferation	[PMID: 10743948]
HOS	IC₅₀	149 μM Compound: Olomoucine	In vitro cytotoxic effect on HOS cancer cell line In vitro cytotoxic effect on HOS cancer cell line	[PMID: 12392733]
HOS	IC₅₀	144 μM Compound: olomoucine	Antiproliferative activity against HOS cell line Antiproliferative activity against HOS cell line	[PMID: 17064068]
K562	IC₅₀	>167 μM Compound: Olomoucine	In vitro cytotoxic effect on K562 cancer cell line In vitro cytotoxic effect on K562 cancer cell line	[PMID: 12392733]
K562	IC₅₀	163 μM Compound: Olomoucine	In vitro antiproliferative activity against myeloid leukemia K562 cell line In vitro antiproliferative activity against myeloid leukemia K562 cell line	[PMID: 12941318]
K562	IC₅₀	145 μM Compound: olomoucine	Antiproliferative activity against K562 cell line Antiproliferative activity against K562 cell line	[PMID: 17064068]
K562	IC₅₀	89.3 μM Compound: Olomucine	Cytotoxicity against human K562 cells after 48 hrs by SRB assay Cytotoxicity against human K562 cells after 48 hrs by SRB assay	[PMID: 20045224]
K562	IC₅₀	163 μM Compound: Olomoucine	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 29273417]
MCF7	IC₅₀	132 μM Compound: Olomoucine	In vitro cytotoxic effect on MCF-7 cancer cell line In vitro cytotoxic effect on MCF-7 cancer cell line	[PMID: 12392733]
MCF7	IC₅₀	134 μM Compound: olomoucine	Antiproliferative activity against MCF7 cell line Antiproliferative activity against MCF7 cell line	[PMID: 17064068]
MCF7	IC₅₀	55.9 μM Compound: Olomucine	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 20045224]
MCF7	IC₅₀	130 μM Compound: 5	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 22819191]
MCF7	IC₅₀	142 μM Compound: Olomoucine	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 to 48 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 to 48 hrs by CCK8 assay	[PMID: 23933045]
NCI-H460	IC₅₀	132 μM Compound: Olomoucine	Cytotoxicity against human H460 cells assessed as growth inhibition after 24 to 48 hrs by CCK8 assay Cytotoxicity against human H460 cells assessed as growth inhibition after 24 to 48 hrs by CCK8 assay	[PMID: 23933045]
Oocyte	IC₅₀	7 μM Compound: olomoucine	In vitro inhibitory activity against Cyclin-dependent kinase 1-cyclin B complex from starfish oocytes In vitro inhibitory activity against Cyclin-dependent kinase 1-cyclin B complex from starfish oocytes	[PMID: 10753466]
Oocyte	IC₅₀	7 μM Compound: Olomoucine (table 2 Page 6846)	Inhibitory concentration against CDK1/Cyclin B complex from Marthasterias glacialis M-phase oocytes Inhibitory concentration against CDK1/Cyclin B complex from Marthasterias glacialis M-phase oocytes	[PMID: 16250643]
Oocyte	IC₅₀	6 μM Compound: 13	Inhibitory activity against purified cdc2 p34/Cyclin B obtained from M phase oocytes of the starfish Marthasterias glacialis. Inhibitory activity against purified cdc2 p34/Cyclin B obtained from M phase oocytes of the starfish Marthasterias glacialis.	[PMID: 9046330]
PC-3	IC₅₀	81 μM Compound: Olomucine	Cytotoxicity against human PC3 cells after 48 hrs by SRB assay Cytotoxicity against human PC3 cells after 48 hrs by SRB assay	[PMID: 20045224]
Sf21	IC₅₀	7 μM Compound: Olomoucine	Inhibition of human recombinant CDK2/cyclin A expressed in baculovirus-infected insect Sf21 cells after 10 mins Inhibition of human recombinant CDK2/cyclin A expressed in baculovirus-infected insect Sf21 cells after 10 mins	[PMID: 20045222]
Sf21	IC₅₀	45 μM Compound: Olomoucine	Inhibition of CDK4/cyclin D expressed in baculovirus infected insect Sf21 cells using [gamma-P32]ATP and histone H1 as substrate after 10 mins by radiometric assay Inhibition of CDK4/cyclin D expressed in baculovirus infected insect Sf21 cells using [gamma-P32]ATP and histone H1 as substrate after 10 mins by radiometric assay	[PMID: 22000924]
Sf21	IC₅₀	7 μM Compound: Olomoucine	Inhibition of CDK2/cyclin A expressed in baculovirus infected insect Sf21 cells using [gamma-P32]ATP and histone H1 as substrate after 10 mins by radiometric assay Inhibition of CDK2/cyclin A expressed in baculovirus infected insect Sf21 cells using [gamma-P32]ATP and histone H1 as substrate after 10 mins by radiometric assay	[PMID: 22000924]
Sf21	IC₅₀	7 μM Compound: Olomoucine	Inhibition of human N-terminal hexahistidine-tagged CDK2 expressed in baculovirus infected Sf21 cells using histone H1 as substrate after 10 mins in presence of [gamma-32P]-ATP Inhibition of human N-terminal hexahistidine-tagged CDK2 expressed in baculovirus infected Sf21 cells using histone H1 as substrate after 10 mins in presence of [gamma-32P]-ATP	[PMID: 23933045]
SK-LU-1	IC₅₀	68.1 μM Compound: Olomucine	Cytotoxicity against human SK-LU-1 cells after 48 hrs by SRB assay Cytotoxicity against human SK-LU-1 cells after 48 hrs by SRB assay	[PMID: 20045224]
SNU-638	GI₅₀	12.05 μM Compound: Olomoucine	Growth inhibition of human HCT116 cells after 2 days by SRB assay Growth inhibition of human HCT116 cells after 2 days by SRB assay	[PMID: 22000924]
SNU-638	GI₅₀	16.62 μM Compound: Olomoucine	Growth inhibition of human SNU638 cells after 2 days by SRB assay Growth inhibition of human SNU638 cells after 2 days by SRB assay	[PMID: 22000924]
U-251	IC₅₀	81.5 μM Compound: Olomucine	Cytotoxicity against human U251 cells after 48 hrs by SRB assay Cytotoxicity against human U251 cells after 48 hrs by SRB assay	[PMID: 20045224]

体外実験

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^[1].
Olomoucine (0, 5, 10, 15, and 25 μM) is a competitive inhibitor for ATP and as a non-competitive inhibitor for histone H^[1].
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^[2].
Olomoucine (0-100 μM) inhibits Gl/S transition of non-small cell lung cancer cell line MB65 cells^[2].
Olomoucine (0-150 μM) inhibits prophase/metaphase transition of Rdditapes oocytes^[2].
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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Olomoucine (8 mg/kg; i.v.; once daily; 7 d) induces apoptosis in tumor cells on the 3rd day after treatment without side effects^[3].
Cassette dosing was found to overestimate the AUC while underestimating the Cmax compared with single dosing administration^[4].

Cassette dosing pharmacokinetics for olomoucine^[4]

Administration	C_max (nM)	Cl_obs (l/h)	V_ss(obs) (l)	MRT_last (h)	AUC_inf(obs) (nM^.h)	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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Dog with spontaneous melanoma (oral and maxillofacial tumors)^[3]
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))^[4]
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).

化学情報

CAS 番号 101622-51-9
性状 Solid
分子量 298.34
分子式 C₁₅H₁₈N₆O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (1)

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Environ Sci Technol

Azocyclotin Binds CDK4 to Disrupt DNA Methylation in Zebrafish Epigenetic Transgenerational Inheritance. [Abstract]

2025 Dec 23;59(50):27130-27142. PMID: 41359812

溶剤 & 溶解度

体外:

DMSO : 66.67 mg/mL (223.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (8.38 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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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). [Content Brief]

[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). [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3519 mL	16.7594 mL	33.5188 mL	83.7970 mL
	5 mM	0.6704 mL	3.3519 mL	6.7038 mL	16.7594 mL
	10 mM	0.3352 mL	1.6759 mL	3.3519 mL	8.3797 mL
	15 mM	0.2235 mL	1.1173 mL	2.2346 mL	5.5865 mL
	20 mM	0.1676 mL	0.8380 mL	1.6759 mL	4.1899 mL
	25 mM	0.1341 mL	0.6704 mL	1.3408 mL	3.3519 mL
	30 mM	0.1117 mL	0.5586 mL	1.1173 mL	2.7932 mL
	40 mM	0.0838 mL	0.4190 mL	0.8380 mL	2.0949 mL
	50 mM	0.0670 mL	0.3352 mL	0.6704 mL	1.6759 mL
	60 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	80 mM	0.0419 mL	0.2095 mL	0.4190 mL	1.0475 mL
	100 mM	0.0335 mL	0.1676 mL	0.3352 mL	0.8380 mL

Keywords

Olomoucine

1 Cited Publications

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Olomoucine

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MedChemExpress（MCE）の使用を引用している文献 Olomoucine

CDK アイソフォーム固有の製品をすべて表示

生物活性

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Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Olomoucine

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Food-Sourced Compound Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

MedChemExpress（MCE）の使用を引用している文献 Olomoucine

CDK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Olomoucine 関連分類

製品番号: HY-W011428