Art. -Nr.: HY-136579

ASN007

(Synonyms: ERK-IN-3)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC₅₀ values. ASN007 exhibits significant anti proliferative activity against various tumor cells. ASN007 can be used for the research of cancers driven by RAS mutations.

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Reinheit: 99.48%
CAS. Nr.: 2055597-12-9
Formel: C₂₂H₂₅ClFN₇O₂
Molecular Weight:473.93

Speicherung:

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

ASN007 Chemical Structure

CAS. Nr.: 2055597-12-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ERK1

ERK2

Alle ERK Isoform-spezifische Produkte anzeigen :

In Vitro

ASN007 (ERK-IN-3) 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].
ASN007 (0.0005-10 µM, 60 min) can selectively inhibit ERK1/ERK2 enzymes (IC₅₀ = 2 nM)^[2].
ASN007 (4 h) dose dependently inhibits RSK1 (Ser380) phosphorylation in HT-29 cells^[2].
ASN007 (15 min-72 h) rapidly (15 minutes) and persistently (72 hours) inhibits p-MSK1 and p-RSK1 in HT-29 cells^[2].
ASN007 (0.0005-10 µM, 72 h) is sensitive to RAS/RAF mutant cell lines (median IC₅₀ = 37 nM)^[2].
ASN007 (24-72 h) can induce G0/G1 phase cell cycle arrest in various cells^[2].

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

In Vivo

ASN007 (ERK-IN-3) (40 mg/kg, p.o., once daily) significantly inhibits tumor growth and has good tolerance at effective doses in nude mice bearing multiple BRAF and KRAS mutant xenograft tumors^[2].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 2055597-12-9
Appearance Solid
Molecular Weight 473.93
Formel C₂₂H₂₅ClFN₇O₂
Color White to light yellow
SMILES

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

ERK-IN-3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (7)

All In Vivo Efficacy StudyWBCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Commun

Supporting cells orchestrate noise-induced hearing loss via a Gasdermin D-dependent signaling loop with hair cells. [Abstract]

2025 Dec 17;16(1):11181. PMID: 41407982
Phytomedicine

Hypocrellin A against intrahepatic Cholangiocarcinoma via multi-target inhibition of the PI3K-AKT-mTOR, MAPK, and STAT3 signaling pathways. [Abstract]

2024 Dec:135:156022. PMID: 39284270

ASN007 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2024 Dec:135:156022. [Abstract]

ASN007 (0-60 μM; 24 h) showed antiproliferative activity and had an IC₅₀ of 17.23 μM for RBE and 25.67 μM for HuccT1 cells.
NPJ Precis Oncol

High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]

2026 Apr 8;10(1):211. PMID: 41951768
Antioxidants (Basel)

Ellagic Acid Reduces Cadmium Exposure-Induced Apoptosis in HT22 Cells via Inhibiting Oxidative Stress and Mitochondrial Dysfunction and Activating Nrf2/HO-1 Pathway. [Abstract]

2024 Oct 25;13(11):1296. PMID: 39594438

ASN007 purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Oct 25;13(11):1296. [Abstract]

ASN007 (0, 5, 10 μM; a duration of 2 h; co-treated with CdSO4 at a concentration of 10 μM for an additional 24 h) did not affect CdSO4-induced cytotoxicity in HT22 cells.
Biomed Mater

Dual-engineered small extracellular vesicles targeted delivery miR-126 for reducing age-related bone loss. [Abstract]

2026 Jul 13;21(4). PMID: 42309139
BJA Open

The concerted actions of microRNA-29a and interferon-β modulate complete Freund's adjuvant-induced inflammatory pain by regulating the expression of type 1 interferon receptor, interferon-stimulated gene 15, and p-extracellular signal-regulated kinase. [Abstract]

2025 Feb 3:13:100376. PMID: 39980495

ASN007 purchased from MedChemExpress. Usage Cited in: BJA Open. 2025 Feb 3:13:100376. [Abstract]

ASN007 (30 μg; intrathecal (i.t.) injection) reversed the mechanical hyperalgesia induced by the miR-29a mimic for 1 h in rats.

ASN007 purchased from MedChemExpress. Usage Cited in: BJA Open. 2025 Feb 3:13:100376. [Abstract]

ASN007 (30 μg; intrathecal (i.t.) injection) showed no effect on the p-ERK and IFNR1 expression. While miR-29a mimic significantly increased the expression of p-ERK and decreased the expression of type 1 interferon receptor (IFNR1) in rats.
Preprints

2024 Sep 11.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (211.00 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

2.1100 mL

10.5501 mL

21.1002 mL

5 mM

0.4220 mL

2.1100 mL

4.2200 mL

10 mM

0.2110 mL

1.0550 mL

2.1100 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (4.39 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 (4.39 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 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 (4.39 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.

Working Solution

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: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 6.67 mg/mL (14.07 mM); Suspended solution; Need ultrasonic

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

Verweise

[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).

[2]. Portelinha A, et al. ASN007 is a selective ERK1/2 inhibitor with preferential activity against RAS-and RAF-mutant tumors. Cell Rep Med. 2021 Jul 21;2(7):100350. [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	2.1100 mL	10.5501 mL	21.1002 mL	52.7504 mL
	5 mM	0.4220 mL	2.1100 mL	4.2200 mL	10.5501 mL
	10 mM	0.2110 mL	1.0550 mL	2.1100 mL	5.2750 mL
	15 mM	0.1407 mL	0.7033 mL	1.4067 mL	3.5167 mL
	20 mM	0.1055 mL	0.5275 mL	1.0550 mL	2.6375 mL
	25 mM	0.0844 mL	0.4220 mL	0.8440 mL	2.1100 mL
	30 mM	0.0703 mL	0.3517 mL	0.7033 mL	1.7583 mL
	40 mM	0.0528 mL	0.2638 mL	0.5275 mL	1.3188 mL
	50 mM	0.0422 mL	0.2110 mL	0.4220 mL	1.0550 mL
	60 mM	0.0352 mL	0.1758 mL	0.3517 mL	0.8792 mL
	80 mM	0.0264 mL	0.1319 mL	0.2638 mL	0.6594 mL
	100 mM	0.0211 mL	0.1055 mL	0.2110 mL	0.5275 mL

Keywords

ASN007

7 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) ASN007

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASN007 Related Classifications

HY-136579 Related Classifications