ERK-IN-3 benzenesulfonate (Synonyms: ERK-IN-3 benzenesulfonate) |
| Catalog No.GC63459 |
ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2055597-39-0
Sample solution is provided at 25 µL, 10mM.
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ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations[1].
ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines[1].ERK-IN-3 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines[1].
ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses[1].
[1]. Sanjeeva PR, et, al. Abstract B150: ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. Molecular Cancer Therapeutics. 2018 Jan; 17(1).
| Cas No. | 2055597-39-0 | SDF | |
| Synonyms | ERK-IN-3 benzenesulfonate | ||
| Formula | C28H31ClFN7O5S | M.Wt | 632.11 |
| Solubility | DMSO : 320 mg/mL (506.24 mM; Need ultrasonic) | Storage | -20°C, away from moisture |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.582 mL | 7.91 mL | 15.82 mL |
| 5 mM | 0.3164 mL | 1.582 mL | 3.164 mL |
| 10 mM | 0.1582 mL | 0.791 mL | 1.582 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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