2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. ERK Apoptosis
  4. ASTX029

ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity.

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

ASTX029 Chemical Structure

ASTX029 Chemical Structure

CAS No. : 2095719-92-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 300 In-stock
50 mg USD 540 In-stock
100 mg USD 950 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

ASTX029 Related Antibodies

Top Publications Citing Use of Products

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity[1][2].

IC50 & Target[1]

ERK1

 

ERK2

 

In Vitro

ASTX029 (96 h) inhibits the proliferation of human cancer cells with MAPK-activating mutations, with IC50 values of 1.8 to 380 nM[2].
ASTX029 (2 h) inhibits the phosphorylation of RSK in both A375 and HCT116 cells, with IC50 values of 3.3 and 4 nM respectively, and also reduces pERK level[2].
ASTX029 (10 and 100 nM, 0-72 h) induces cell-cycle to arrest in the G1-phase, and induces cell apoptosis in A375 and HCT116 cells[2].

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

ASTX029 Related Antibodies

Western Blot Analysis[2]

Cell Line: A375 and HCT116 cells
Concentration: 1 nM-100 nM
Incubation Time: 2 h
Result: Decreased pRSK and pERK.

Apoptosis Analysis[2]

Cell Line: A375 and HCT116 cells
Concentration: 0-100 nM
Incubation Time: 0-72 h
Result: Arrested cell in the G1-phase.
Increased cleaved PARP and Bim protein level.
In Vivo

ASTX029 (20-75 mg/kg, p.o.) inhibits tumor growth in Colo205 (BRAFV600E-mutant colorectal cancer) tumor-bearing mice[2].
ASTX029 (5 mg/kg, p.o., mice) shows AUC of 1600 ng h/mL, T1/2 of 2.9 h, F (%) of 42%[3].

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

Animal Model: Colo205, A375, Calu-6, HCC44, HCT116 or MA-MEL-28 xenografts tumor-bearing mice[2]
Dosage: 75 mg/kg
Administration: p.o., once daily
Result: Inhibited tumor growth in various tumor models.
Clinical Trial
Molecular Weight

584.04

Formula

C29H31ClFN5O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C(C1=CC2=C(CN([C@H](C)C(N[C@H](CO)C3=CC(F)=CC(OC)=C3)=O)C2=O)C=C1)=N4)=CN=C4NC5CCOCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (428.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7122 mL 8.5611 mL 17.1221 mL
5 mM 0.3424 mL 1.7122 mL 3.4244 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 2.08 mg/mL (3.56 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.
  • Protocol 2

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

    Solubility: 2.08 mg/mL (3.56 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.82%

COA (251 KB) HNMR (293 KB) LCMS (264 KB)

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. 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 1.7122 mL 8.5611 mL 17.1221 mL 42.8053 mL
5 mM 0.3424 mL 1.7122 mL 3.4244 mL 8.5611 mL
10 mM 0.1712 mL 0.8561 mL 1.7122 mL 4.2805 mL
15 mM 0.1141 mL 0.5707 mL 1.1415 mL 2.8537 mL
20 mM 0.0856 mL 0.4281 mL 0.8561 mL 2.1403 mL
25 mM 0.0685 mL 0.3424 mL 0.6849 mL 1.7122 mL
30 mM 0.0571 mL 0.2854 mL 0.5707 mL 1.4268 mL
40 mM 0.0428 mL 0.2140 mL 0.4281 mL 1.0701 mL
50 mM 0.0342 mL 0.1712 mL 0.3424 mL 0.8561 mL
60 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7134 mL
80 mM 0.0214 mL 0.1070 mL 0.2140 mL 0.5351 mL
100 mM 0.0171 mL 0.0856 mL 0.1712 mL 0.4281 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

ASTX029 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:

ASTX0292095719-92-7ASTX 029ASTX-029ERKApoptosisExtracellular signal regulated kinasesA375HCT116tumoranticancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ASTX029
Cat. No.:
HY-126288
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.