MAPK-IN-2

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 (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT 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 (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM) [1].

Product Specifications

UNSPSC

12352005

Target

CDK; c-Met/HGFR; EGFR; p38 MAPK; Raf

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mapk-in-2.html

Purity

98.54

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C20H11Cl2N3O

Molecular Weight

380.23

References & Citations

[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.