ERK5-IN-2 |
| Catalog No.GC36002 |
ERK5-IN-2 es un inhibidor selectivo de ERK5 submicromolar activo por vÍa oral con IC50 de 0,82 μM, 3 μM para ERK5 y ERK5 MEF2D, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1888305-96-1
Sample solution is provided at 25 µL, 10mM.
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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[1]. ERK5|0.82 μM (IC50)|ERK5 MEF2D|3 μM (IC50)
ERK5-IN-2 (compound 46) (p.o.; 100mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin[1]. ERK5-IN-2 (i.v. or p.o.; 10mg/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]. 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]
[1]. Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543.
| Cas No. | 1888305-96-1 | SDF | |
| Canonical SMILES | FC1=CC=CC(Br)=C1C(C2=CNC(C(NC3=CC=CN=C3)=O)=C2)=O | ||
| Formula | C17H11BrFN3O2 | M.Wt | 388.19 |
| Solubility | DMSO: 250 mg/mL (644.01 mM) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5761 mL | 12.8803 mL | 25.7606 mL |
| 5 mM | 0.5152 mL | 2.5761 mL | 5.1521 mL |
| 10 mM | 0.2576 mL | 1.288 mL | 2.5761 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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