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5mg |
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25mg |
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50mg |
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100mg |
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500mg |
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Purity: ≥98%
Olomoucine, a purine derivative, is a novel and potent CDK (cyclin-dependent kinases) inhibitor that competes for the ATP binding site of the kinase and induces G arrest.. Olomoucine has been demonstrated to reversibly stop cycling Arabidopsis cells in late G1 and G2, as well as differentiated Petunia cells that have been induced to divide at the G1 phase.
Targets |
cdk2-cyclin A (IC50 = 7 μM); cdk2-cyclin E (IC50 = 7 μM); cdk5-p35 (IC50 = 25 μM)
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ln Vitro |
Olomoucine suppresses the kinases CDK2 and CDC2, with IC50 values of 7 μM for CDC2/cyclin B, 7 μM for CDK2/cyclin A, 7 μM for CDK2/cyclin E, 3 μm for CDK5/p35, and 25 μM for ERK1/p44 MAPK, respectively[1].
Olomoucine is a non-competitive inhibitor of histone H and a competitive inhibitor of ATP at concentrations of 0, 5, 10, 15, and 25 μM[1]. Olomoucine (0-1000 μM) causes a Gl arrest akin to interleukin-2 deprivation and suppresses DNA synthesis in interleukin-2-stimulated T lymphocytes (CTLL-2 cells)[2]. Olomoucine (0-100 μM) inhibits the MB65 cell line's Gl/S transition in non-small cell lung cancer[2]. Olomoucine (0-150 μM) inhibits the Rdditapes oocytes' prophase/metaphase transition[2]. Olomoucine has been shown to inhibit the survival of tumor cells, with IC50s of 32.35 μM for dog melanoma, 42.15 μM for mouse B16 melanoma, and 82.30 μM for human melanoma, respectively[3]. |
ln Vivo |
Olomoucine (8 mg/kg; i.v.; once daily; 7 d) causes tumor cells to undergo apoptosis without causing any side effects on the third day following treatment[3].
It has been discovered that, in comparison to single dosage administration, cassette dosing underestimates the Cmax and overestimates the AUC[4]. |
Animal Protocol |
Dog with spontaneous melanoma (oral and maxillofacial tumors)[3]
8 mg/kg Intravenous injection; once daily; for 7 days |
References |
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Molecular Formula |
C15H18N6O
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Molecular Weight |
298.34302
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Exact Mass |
298.15
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Elemental Analysis |
C, 60.39; H, 6.08; N, 28.17; O, 5.36
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CAS # |
101622-51-9
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Related CAS # |
101622-51-9
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Appearance |
Solid powder
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SMILES |
CN1C=NC2=C(N=C(N=C21)NCCO)NCC3=CC=CC=C3
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InChi Key |
GTVPOLSIJWJJNY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H18N6O/c1-21-10-18-12-13(17-9-11-5-3-2-4-6-11)19-15(16-7-8-22)20-14(12)21/h2-6,10,22H,7-9H2,1H3,(H2,16,17,19,20)
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Chemical Name |
2-[[6-(benzylamino)-9-methylpurin-2-yl]amino]ethanol
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Synonyms |
Olomoucine
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~66.7 mg/mL (~223.5 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.38 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.