Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
MEK1 31 nM (DC50, in HT29 cells) MEK2 17 nM (DC50, in HT29 cells) MEK1 31 nM (DC50, in SK-MEL-28 cells) MEK2 9.3 nM (DC50, in SK-MEL-28 cells)
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ln Vitro |
Compound 23, or MS432, has the ability to significantly lower the levels of MEK1/2 protein in COLO 205 cells (DC50 (MEK1) = 18±7 nM, DC50 (MEK2) = 11±2 nM) and UACC257 cells (DC50 (MEK1) = 56±25 nM, DC50 (MEK2) = 27±19 nM).
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ln Vivo |
In evaluated cancer cell lines, MS432 (Compound 23) demonstrated good plasma exposure, with GI50 values that were roughly 3 to 20 times greater than Compound 23[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: (HT-29, SK-MEL-28, COLO 205 and UACC 257 cell lines. Tested Tested Concentrations: 0-1 μM. Incubation Duration: 72 hrs (hours). Experimental Results: Effectively inhibited proliferation of these CRC and melanoma cells in a concentration-dependent manner, with GI50 values ranging from 30 to 200 nM. |
Animal Protocol |
Animal/Disease Models: Male Swiss Albino mice[1].
Doses: 50 mg/kg (pharmacokinetic/PK Analysis). Route of Administration: IP Experimental Results: Displays good plasma exposure with the maximum plasma concentration of 1,400 nM detected at 0.5 hour post dosing and plasma concentration of 710 nM at 8 hrs (hours) post dosing. |
References |
[1]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019 Dec 12;62(23):10897-10911.
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Molecular Formula |
C50H65F3IN7O6S
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Molecular Weight |
1076.06
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CAS # |
2672512-44-4
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Related CAS # |
PD0325901-O-C2-dioxolane;2581116-22-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(N1C[C@@H](C[C@H]1C(=O)N[C@H](C1C=CC(C2=C(N=CS2)C)=CC=1)C)O)(=O)[C@H](C(C)(C)C)NC(=O)CCCCCCCCCCNCCCONC(C1C=CC(=C(C=1NC1C=CC(=CC=1F)I)F)F)=O
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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 (92.93 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.32 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.9293 mL | 4.6466 mL | 9.2932 mL | |
5 mM | 0.1859 mL | 0.9293 mL | 1.8586 mL | |
10 mM | 0.0929 mL | 0.4647 mL | 0.9293 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.