ASTX029

Name: ASTX029
Brand: MedChemExpress
SKU: HY-126288
Rating: 5.0 (4 reviews)

Cat. No.: HY-126288 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2095719-92-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 154	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 154	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE ASTX029

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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

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.

Clinical Trial

Molecular Weight

584.04

Formula

C₂₉H₃₁ClFN₅O₅

CAS No.

2095719-92-7

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
10 mM	0.1712 mL	0.8561 mL	1.7122 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
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

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

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

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

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

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ASTX029

Customer Review

ASTX029 Related Antibodies

4 Publications Citing Use of MCE ASTX029

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ERK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ASTX029 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ASTX029 Related Classifications

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