Olomoucine
Based on 1 publication(s) in Google Scholar
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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- Pureza: 99.88%
- No. CAS: 101622-51-9
- Fòrmula: C15H18N6O
- Peso molecular:298.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Olomoucine
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Actividad biológica
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cdk2-cyclin A 7 μM (IC50) |
cdk2-cyclin E 7 μM (IC50) |
cdk5-p35 25 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | GI50 |
16.6 μM
Compound: Olomoucine
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Growth inhibition of human A431 cells after 2 days by SRB assay
Growth inhibition of human A431 cells after 2 days by SRB assay
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[PMID: 22000924] |
| A549 | IC50 |
57 μg/mL
Compound: Olomoucine
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Inhibition of A549 cancer cell proliferation
Inhibition of A549 cancer cell proliferation
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[PMID: 10743948] |
| A549 | IC50 |
130 μM
Compound: Olomoucine
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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
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[PMID: 23933045] |
| B16-F10 | IC50 |
105 μM
Compound: 5
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Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay
Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay
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[PMID: 22819191] |
| CCRF-CEM | IC50 |
62 μM
Compound: Olomoucine
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In vitro cytotoxic effect on CEM cancer cell line
In vitro cytotoxic effect on CEM cancer cell line
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[PMID: 12392733] |
| COLO1 | IC50 |
87 μg/mL
Compound: Olomoucine
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Inhibition of Col1 cancer cell proliferation
Inhibition of Col1 cancer cell proliferation
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[PMID: 10743948] |
| G-361 | IC50 |
160 μM
Compound: Olomoucine
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In vitro cytotoxic effect on G361 cancer cell line
In vitro cytotoxic effect on G361 cancer cell line
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[PMID: 12392733] |
| G-361 | IC50 |
147 μM
Compound: olomoucine
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Antiproliferative activity against G361 cell line
Antiproliferative activity against G361 cell line
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[PMID: 17064068] |
| HCT-15 | IC50 |
62.5 μM
Compound: Olomucine
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Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay
Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay
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[PMID: 20045224] |
| HeLa S3 | GI50 |
65 μM
Compound: 1
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Antiproliferative activity against human HeLaS3 cells by sulforhodamine B assay
Antiproliferative activity against human HeLaS3 cells by sulforhodamine B assay
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[PMID: 19846305] |
| HL-60 | IC50 |
50 μg/mL
Compound: Olomoucine
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Inhibition of HL60 cancer cell proliferation
Inhibition of HL60 cancer cell proliferation
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[PMID: 10743948] |
| HOS | IC50 |
149 μM
Compound: Olomoucine
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In vitro cytotoxic effect on HOS cancer cell line
In vitro cytotoxic effect on HOS cancer cell line
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[PMID: 12392733] |
| HOS | IC50 |
144 μM
Compound: olomoucine
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Antiproliferative activity against HOS cell line
Antiproliferative activity against HOS cell line
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[PMID: 17064068] |
| K562 | IC50 |
>167 μM
Compound: Olomoucine
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In vitro cytotoxic effect on K562 cancer cell line
In vitro cytotoxic effect on K562 cancer cell line
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[PMID: 12392733] |
| K562 | IC50 |
163 μM
Compound: Olomoucine
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In vitro antiproliferative activity against myeloid leukemia K562 cell line
In vitro antiproliferative activity against myeloid leukemia K562 cell line
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[PMID: 12941318] |
| K562 | IC50 |
145 μM
Compound: olomoucine
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Antiproliferative activity against K562 cell line
Antiproliferative activity against K562 cell line
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[PMID: 17064068] |
| K562 | IC50 |
89.3 μM
Compound: Olomucine
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Cytotoxicity against human K562 cells after 48 hrs by SRB assay
Cytotoxicity against human K562 cells after 48 hrs by SRB assay
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[PMID: 20045224] |
| K562 | IC50 |
163 μM
Compound: Olomoucine
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Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
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[PMID: 29273417] |
| MCF7 | IC50 |
132 μM
Compound: Olomoucine
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In vitro cytotoxic effect on MCF-7 cancer cell line
In vitro cytotoxic effect on MCF-7 cancer cell line
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[PMID: 12392733] |
| MCF7 | IC50 |
134 μM
Compound: olomoucine
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Antiproliferative activity against MCF7 cell line
Antiproliferative activity against MCF7 cell line
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[PMID: 17064068] |
| MCF7 | IC50 |
55.9 μM
Compound: Olomucine
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Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
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[PMID: 20045224] |
| MCF7 | IC50 |
130 μM
Compound: 5
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Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
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[PMID: 22819191] |
| MCF7 | IC50 |
142 μM
Compound: Olomoucine
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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
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[PMID: 23933045] |
| NCI-H460 | IC50 |
132 μM
Compound: Olomoucine
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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
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[PMID: 23933045] |
| Oocyte | IC50 |
7 μM
Compound: olomoucine
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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
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[PMID: 10753466] |
| Oocyte | IC50 |
7 μM
Compound: Olomoucine (table 2 Page 6846)
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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
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[PMID: 16250643] |
| Oocyte | IC50 |
6 μM
Compound: 13
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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.
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[PMID: 9046330] |
| PC-3 | IC50 |
81 μM
Compound: Olomucine
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Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
Cytotoxicity against human PC3 cells after 48 hrs by SRB assay
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[PMID: 20045224] |
| Sf21 | IC50 |
7 μM
Compound: Olomoucine
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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
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[PMID: 20045222] |
| Sf21 | IC50 |
45 μM
Compound: Olomoucine
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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
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[PMID: 22000924] |
| Sf21 | IC50 |
7 μM
Compound: Olomoucine
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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
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[PMID: 22000924] |
| Sf21 | IC50 |
7 μM
Compound: Olomoucine
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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
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[PMID: 23933045] |
| SK-LU-1 | IC50 |
68.1 μM
Compound: Olomucine
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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
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[PMID: 20045224] |
| SNU-638 | GI50 |
12.05 μM
Compound: Olomoucine
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Growth inhibition of human HCT116 cells after 2 days by SRB assay
Growth inhibition of human HCT116 cells after 2 days by SRB assay
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[PMID: 22000924] |
| SNU-638 | GI50 |
16.62 μM
Compound: Olomoucine
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Growth inhibition of human SNU638 cells after 2 days by SRB assay
Growth inhibition of human SNU638 cells after 2 days by SRB assay
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[PMID: 22000924] |
| U-251 | IC50 |
81.5 μM
Compound: Olomucine
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Cytotoxicity against human U251 cells after 48 hrs by SRB assay
Cytotoxicity against human U251 cells after 48 hrs by SRB assay
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[PMID: 20045224] |
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.
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) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dog with spontaneous melanoma (oral and maxillofacial tumors)[3]
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Dosage:8 mg/kg
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Administration:Intravenous injection; once daily; for 7 days
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Result:Induced programmed cell death of cancer cells and resulted in rapid eradication of at least 68% of the tumor cells.
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Animal Model:Female Balb C− mice (6 weeks of age; weight of 20 g (±1.2 g))[4]
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Dosage:50 mg/kg (single agent) or 16.6 mg/kg combinded with purines (cassette)
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Administration:Intravenous injection (tail vein); samples taken at 0.25, 0.5, 1, 2, 4, 6, and 24 h post-dosing
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Result:Resulted faster plasma concentration decreasing with 50 mg/kg (as single agent) than 16.6 mg/kg (as cassette).
Chemical Information
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No. CAS 101622-51-9
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Appearance Solid
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Peso molecular 298.34
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Fòrmula C15H18N6O
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Color White to off-white
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SMILES
CN1C=NC2=C(NCC3=CC=CC=C3)N=C(NCCO)N=C12
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Journal Impact Factor
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Most Recent
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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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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 |
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