Cat. No.: HY-155736

MAPK-IN-2

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MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR^WT IC₅₀=281 nM, c-MET IC₅₀=205 nM, B-RAF^WT IC₅₀=112 nM, and CDK4/6 IC₅₀=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR^T790M IC₅₀=69 nM and B-RAF^V600E IC₅₀=83 nM).

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Pureté: 99.66%
CAS No.: 3052814-46-4
Formule: C₂₀H₁₁Cl₂N₃O
Masse moléculaire:380.23

Stockage:

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

MAPK-IN-2 Chemical Structure

CAS No.: 3052814-46-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 281 nM (EGFR^WT), 69 nM (EGFR^T790M), 205 nM (c-MET), 112 nM (B-RAF^WT), 83 nM (B-RAF^V600E), 95 nM (CDK4), 184 nM (CDK6)^[1]

Voir tous les produits spécifiques à Isoform p38 MAPK :

Voir tous les produits spécifiques à Isoform CDK :

Voir tous les produits spécifiques à Isoform Raf :

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
FHC	GI₅₀	26.84 μM Compound: 3h	Cytotoxicity against human FHC cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human FHC cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]
HCT-116	GI₅₀	2.53 μM Compound: 3h	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]
HEK293	GI₅₀	22.4 μM Compound: 3h	Cytotoxicity against human HEK293 cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human HEK293 cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]
HOP-92	GI₅₀	0.75 μM Compound: 3h	Cytotoxicity against human HOP-92 cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human HOP-92 cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]
MRC5	GI₅₀	28.48 μM Compound: 3h	Cytotoxicity against human MRC5 cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human MRC5 cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]
RXF 393	GI₅₀	3.12 μM Compound: 3h	Cytotoxicity against human RXF 393 cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human RXF 393 cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]
SR	GI₅₀	2.77 μM Compound: 3h	Cytotoxicity against human SR cells assessed as cell growth inhibition incubated for 4 days by MTT assay Cytotoxicity against human SR cells assessed as cell growth inhibition incubated for 4 days by MTT assay	[PMID: 37506545]

Chemical Information

CAS No. 3052814-46-4
Appearance Solid
Masse moléculaire 380.23
Formule C₂₀H₁₁Cl₂N₃O
Color Light yellow to orange
SMILES

O=C1C(C#N)=C(C2=CC=C(Cl)C=C2Cl)C=C(C3=CNC4=C3C=CC=C4)N1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 16.67 mg/mL (43.84 mM; ultrasonic and warming and heat to 60°C; 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

2.6300 mL

13.1499 mL

26.2999 mL

5 mM

0.5260 mL

2.6300 mL

5.2600 mL

10 mM

0.2630 mL

1.3150 mL

2.6300 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: 1.67 mg/mL (4.39 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.67 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 (16.7 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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Saleh MM, et al. The mystery of titan hunter: Rationalized striking of the MAPK pathway via Newly synthesized 6-Indolylpyridone-3-Carbonitrile derivatives. Eur J Med Chem. 2023 Nov 5;259:115675. [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	2.6300 mL	13.1499 mL	26.2999 mL	65.7497 mL
	5 mM	0.5260 mL	2.6300 mL	5.2600 mL	13.1499 mL
	10 mM	0.2630 mL	1.3150 mL	2.6300 mL	6.5750 mL
	15 mM	0.1753 mL	0.8767 mL	1.7533 mL	4.3833 mL
	20 mM	0.1315 mL	0.6575 mL	1.3150 mL	3.2875 mL
	25 mM	0.1052 mL	0.5260 mL	1.0520 mL	2.6300 mL
	30 mM	0.0877 mL	0.4383 mL	0.8767 mL	2.1917 mL
	40 mM	0.0657 mL	0.3287 mL	0.6575 mL	1.6437 mL

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MAPK-IN-2

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform p38 MAPK

Voir tous les produits spécifiques à Isoform CDK

Voir tous les produits spécifiques à Isoform Raf

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MAPK-IN-2 Related Classifications

Cat. No.: HY-155736