Olomoucine

Name: Olomoucine
Brand: MedChemExpress
SKU: HY-W011428
Rating: 4.5 (1 reviews)

Cat. No.: HY-W011428 Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Olomoucine Chemical Structure

CAS No. : 101622-51-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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	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]
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]
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]
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]
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]
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]
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	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 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	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]

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^[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.

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^[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).

Molecular Weight

298.34

Formula

C₁₅H₁₈N₆O

CAS No.

101622-51-9

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.78%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (251 KB) RP-HPLC (245 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Olomoucine Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Olomoucine101622-51-9CDKCyclin dependent kinasecell cycleproliferationprotein kinasescyclindependent kinasescdc2cdk2purines2-(2-hydroxyethylamino)-6-beazylamino-9-metbylpurinexenopus laevis oocytesnon-small cell lung cancer cell lineMR6.5Inhibitorinhibitorinhibit

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Olomoucine

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