| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In comparison to the DMSO control, MS37452 (125-500 μM; 12 hours) significantly elevated INK4A/ARF transcript levels at 250 μM and 500 μM by 25% and 60%, respectively [1]. After two hours of treatment on human PC3 prostate cancer cells, CBX7 occupancy at the INK4A/ARF site is reduced by MS37452 (250 μM) [1]. Compared to DMSO therapy and single drug treatment, the combination of MS37452 (200 µM; 5 days) plus doxorubicin resulted in a prolonged decrease in cell viability [2]. When combined with doxorubicin, MS37452 (200 µM; 5 days)—a CBX7 chromodomain inhibitor (CBX7i)—is a unique treatment approach [2].
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|---|---|
| Cell Assay |
RT-PCR[1]
Cell Types: PC3 Cell Tested Concentrations: 125-500 μM Incubation Duration: 12 hrs (hours) Experimental Results: INK4A/ARF expression was up-regulated by up to 25% and 60% at 250 μM and 500 μM, respectively. Cell viability assay [2] Cell Types: Glioblastoma multiforme (GBM) U118MG Cell Tested Concentrations: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, Temozolomide 50 µM, SAHA 1 µM Incubation Duration: 5 days Experimental Results: Several combinations were identified that resulted in a sustained decrease in cell viability compared to DMSO treatment and single drug treatment (SAHA/TMZ and MS37452/doxorubicin). |
| References |
| Molecular Formula |
C22H26N2O5
|
|---|---|
| Molecular Weight |
398.45
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| Exact Mass |
398.184
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| Elemental Analysis |
C, 66.32; H, 6.58; N, 7.03; O, 20.08
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| CAS # |
423748-02-1
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| PubChem CID |
1072048
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
628.8±55.0 °C at 760 mmHg
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| Flash Point |
334.1±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
2.29
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=CC=C1)OCC(=O)N2CCN(CC2)C(=O)C3=C(C(=CC=C3)OC)OC
|
| InChi Key |
LUMCNRKHZRYQOV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26N2O5/c1-16-6-4-7-17(14-16)29-15-20(25)23-10-12-24(13-11-23)22(26)18-8-5-9-19(27-2)21(18)28-3/h4-9,14H,10-13,15H2,1-3H3
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| Chemical Name |
1-[4-(2,3-dimethoxybenzoyl)piperazin-1-yl]-2-(3-methylphenoxy)ethanone
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| Synonyms |
MS 37452; MS-37452; MS37452
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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 : ~100 mg/mL (~250.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 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 (6.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5097 mL | 12.5486 mL | 25.0973 mL | |
| 5 mM | 0.5019 mL | 2.5097 mL | 5.0195 mL | |
| 10 mM | 0.2510 mL | 1.2549 mL | 2.5097 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.
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