2. Cell Cycle/DNA Damage
  3. CDK
  4. Olomoucine

Olomoucine 

Cat. No.: HY-W011428 Purity: 99.78%
COA Handling Instructions

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

Olomoucine Chemical Structure

CAS No. : 101622-51-9

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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)

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].

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 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.

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

Appearance

Solid

Formula

C15H18N6O
CAS No.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.78%

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

Handling Instructions (2659 KB)
References
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Help & FAQs
  • 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.

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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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