ERK5-IN-2
Based on 1 Customer Validation
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
For research use only. We do not sell to patients.
- Purity: 98.45%
- CAS No.: 1888305-96-1
- Formula: C17H11BrFN3O2
- Molecular Weight:388.19
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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ERK5 0.82 μM (IC50) |
ERK5 MEF2D 3 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
3 μM
Compound: 46
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Inhibition of HA-tagged ERK5 (unknown origin) coexpressed with mutationally activated EGFP-MEK5D and Gal4-MEF2D in HEK293 cells assessed as reduction in MEF2 transcription by measuring luciferase signal after 20 hrs by luciferase reporter gene assay
Inhibition of HA-tagged ERK5 (unknown origin) coexpressed with mutationally activated EGFP-MEK5D and Gal4-MEF2D in HEK293 cells assessed as reduction in MEF2 transcription by measuring luciferase signal after 20 hrs by luciferase reporter gene assay
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[PMID: 31212132] |
| PC-3 | GI50 |
44 μM
Compound: 46
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Growth inhibition of human PC3 cells
Growth inhibition of human PC3 cells
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[PMID: 31212132] |
| Sf9 | IC50 |
0.82 μM
Compound: 46
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Inhibition of recombinant N-terminal His-tagged human ERK5 (2 to 409 residues) co-expressed with GST-tagged human truncated MEK5DD lacking N-terminal 11 residues (13 to 448 residues) in Sf9 insect cells assessed as substrate peptide phosphorylation using
Inhibition of recombinant N-terminal His-tagged human ERK5 (2 to 409 residues) co-expressed with GST-tagged human truncated MEK5DD lacking N-terminal 11 residues (13 to 448 residues) in Sf9 insect cells assessed as substrate peptide phosphorylation using
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[PMID: 31212132] |
ERK5-IN-2 (i.v. or p.o.; 10 mg/kg for 0.083-24 hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2 cell permeability assay in both human and mouse[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 mice (8-10 weeks old) with Matrigel inoculation and female CD1 nude (nu/nu) mice (8-10 weeks old) bearing A2780 human ovarian carcinoma xenografts[1]
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Dosage:100 mg/kg
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Administration:P.o.; twice-daily; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days
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Result:Tumor volumes were significantly reduced.
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Animal Model:Female CD1 mice at 8-10 weeks of age[1]
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Dosage:10 mg/kg
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Administration:I.v. or p.o.; 0.083-24 hours
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Result:The terminal plasma half-life was 38 min, with a plasma clearance of 27 mL/min/kg, and oral bioavailability of 68%.
Chemical Information
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CAS No. 1888305-96-1
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Appearance Solid
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Molecular Weight 388.19
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Formula C17H11BrFN3O2
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Color White to off-white
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SMILES
FC1=CC=CC(Br)=C1C(C2=CNC(C(NC3=CC=CN=C3)=O)=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 250 mg/mL (644.01 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 (protect from light). 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 (protect from light). 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: ≥ 2.08 mg/mL (5.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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 (protect from light). 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 | 2.5761 mL | 12.8803 mL | 25.7606 mL | 64.4015 mL |
| 5 mM | 0.5152 mL | 2.5761 mL | 5.1521 mL | 12.8803 mL | |
| 10 mM | 0.2576 mL | 1.2880 mL | 2.5761 mL | 6.4401 mL | |
| 15 mM | 0.1717 mL | 0.8587 mL | 1.7174 mL | 4.2934 mL | |
| 20 mM | 0.1288 mL | 0.6440 mL | 1.2880 mL | 3.2201 mL | |
| 25 mM | 0.1030 mL | 0.5152 mL | 1.0304 mL | 2.5761 mL | |
| 30 mM | 0.0859 mL | 0.4293 mL | 0.8587 mL | 2.1467 mL | |
| 40 mM | 0.0644 mL | 0.3220 mL | 0.6440 mL | 1.6100 mL | |
| 50 mM | 0.0515 mL | 0.2576 mL | 0.5152 mL | 1.2880 mL | |
| 60 mM | 0.0429 mL | 0.2147 mL | 0.4293 mL | 1.0734 mL | |
| 80 mM | 0.0322 mL | 0.1610 mL | 0.3220 mL | 0.8050 mL | |
| 100 mM | 0.0258 mL | 0.1288 mL | 0.2576 mL | 0.6440 mL |
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