Referencia número: HY-126288

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ASTX029

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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

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Pureza: 99.86%
No. CAS: 2095719-92-7
Fòrmula: C₂₉H₃₁ClFN₅O₅
Peso molecular:584.04

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ASTX029 Chemical Structure

No. CAS: 2095719-92-7

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (7)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

Ver todos los productos específicos de isoformas ERK :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	3.4 nM Compound: 15	Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay	[PMID: 34387469]
COLO 205	IC₅₀	3.6 nM Compound: 15	Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay	[PMID: 34387469]

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.

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 (BRAF^V600E-mutant colorectal cancer) tumor-bearing mice^[2].
ASTX029 (5 mg/kg, p.o., mice) shows AUC of 1600 ng h/mL, T_1/2 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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 2095719-92-7
Appearance Solid
Peso molecular 584.04
Fòrmula C₂₉H₃₁ClFN₅O₅
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

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Adv Sci (Weinh)

ETV4 Promotes Colorectal Cancer Progression by Reprogramming Asparagine Metabolism to Remodel the Stromal Microenvironment. [Abstract]

2026 Mar 20:e16557. PMID: 41861091
J Agric Food Chem

Glycyrrhizic Acid against Mycoplasma gallisepticum-Induced Inflammation and Apoptosis Through Suppressing the MAPK Pathway in Chickens. [Abstract]

2022 Feb 16;70(6):1996-2009. PMID: 35128924
Drug Des Devel Ther

Andrographolide Inhibits Static Mechanical Pressure-Induced Intervertebral Disc Degeneration via the MAPK/Nrf2/HO-1 Pathway. [Abstract]

2023 Feb 20:17:535-550. PMID: 36845666
J Integr Agric

2023 Nov 28.
Int Immunopharmacol

Isoliquiritigenin alleviates neuropathic pain by reducing microglia inflammation through inhibition of the ERK signaling pathway and decreasing CEBPB transcription expression. [Abstract]

2024 Nov 2;143(Pt 3):113536. PMID: 39488922
Int J Mol Sci

Leucine Zipper Downregulated in Cancer-1 Interacts with Clathrin Adaptors to Control Epidermal Growth Factor Receptor (EGFR) Internalization and Gefitinib Response in EGFR-Mutated Non-Small Cell Lung Cancer. [Abstract]

2024 Jan 23;25(3):1374. PMID: 38338651
Patent

US20250110133A1.

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7122 mL

8.5611 mL

17.1221 mL

5 mM

0.3424 mL

1.7122 mL

3.4244 mL

10 mM

0.1712 mL

0.8561 mL

1.7122 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Michael Reader, et al. 6-pyrimidin-isoindole derivative as erk1/2 inhibitor. WO2018193410A1.

[2]. Munck JM, et al. ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK. Mol Cancer Ther. 2021 Oct;20(10):1757-1768. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

ASTX029

7 Cited Publications

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ASTX029

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Immunology/Inflammation Compound Library

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MAPK Compound Library

Stem Cell Signaling Compound Library

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Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) ASTX029

Ver todos los productos específicos de isoformas ERK

Actividad biológica

Chemical Information

Publications (7)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

ASTX029 Related Classifications

HY-126288 Related Classifications