2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. ASN007 benzenesulfonate

ASN007 benzenesulfonate  (Synonyms: ERK-IN-3 benzenesulfonate)

Cat. No.: HY-136579A Purity: 98.06%
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ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations.

For research use only. We do not sell to patients.

ASN007 benzenesulfonate Chemical Structure

ASN007 benzenesulfonate Chemical Structure

CAS No. : 2055597-39-0

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Based on 1 publication(s) in Google Scholar

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ASN007 benzenesulfonate Related Antibodies

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  • Biological Activity

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Description

ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations[1].

IC50 & Target[1]

ERK1

 

ERK2

 

In Vitro

ASN007 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines[1].
ASN007 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ASN007 benzenesulfonate Related Antibodies
In Vivo

ASN007 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

632.11

Formula

C28H31ClFN7O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(C2=NC(NC3CCOCC3)=NC=C2C)C=N1)N[C@@H](C4=CC(F)=CC(Cl)=C4)CN.O=S(C5=CC=CC=C5)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 320 mg/mL (506.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (158.20 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5820 mL 7.9100 mL 15.8200 mL
5 mM 0.3164 mL 1.5820 mL 3.1640 mL
View the 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 8 mg/mL (12.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 8 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (80.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 8 mg/mL (12.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 8 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (80.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (158.20 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 1.5820 mL 7.9100 mL 15.8200 mL 39.5501 mL
5 mM 0.3164 mL 1.5820 mL 3.1640 mL 7.9100 mL
10 mM 0.1582 mL 0.7910 mL 1.5820 mL 3.9550 mL
15 mM 0.1055 mL 0.5273 mL 1.0547 mL 2.6367 mL
20 mM 0.0791 mL 0.3955 mL 0.7910 mL 1.9775 mL
25 mM 0.0633 mL 0.3164 mL 0.6328 mL 1.5820 mL
30 mM 0.0527 mL 0.2637 mL 0.5273 mL 1.3183 mL
40 mM 0.0396 mL 0.1978 mL 0.3955 mL 0.9888 mL
50 mM 0.0316 mL 0.1582 mL 0.3164 mL 0.7910 mL
60 mM 0.0264 mL 0.1318 mL 0.2637 mL 0.6592 mL
80 mM 0.0198 mL 0.0989 mL 0.1978 mL 0.4944 mL
100 mM 0.0158 mL 0.0791 mL 0.1582 mL 0.3955 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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ASN007 benzenesulfonate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ASN0072055597-39-0ERK-IN-3ASN 007ASN-007ERKExtracellular signal regulated kinasesERK1/2cancerRASInhibitorinhibitorinhibit

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