Related Experiment Video

Updated: Oct 26, 2025

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
07:49

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods

Published on: July 17, 2019

6.2K

ASN007 is a selective ERK1/2 inhibitor with preferential activity against RAS-and RAF-mutant tumors

Ana Portelinha1, Scott Thompson2, Roger A Smith2

  • 1Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, NY, USA.

Cell Reports. Medicine
|August 2, 2021
PubMed

Insights

ASN007, a new ERK1/2 inhibitor, shows strong anticancer activity in preclinical models with RAS/RAF mutations. Combining it with PI3K inhibitors enhances its effectiveness in treating resistant cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The RAS/RAF/MEK/ERK signaling pathway is frequently activated in various cancers.
  • Targeting extracellular signal-regulated kinases ERK1 and ERK2 (ERK1/2) is a key therapeutic strategy.
  • Development of novel inhibitors is crucial for overcoming resistance mechanisms.

Purpose of the Study:

  • To characterize ASN007, an orally bioavailable and selective ERK1/2 inhibitor.
  • To evaluate the efficacy of ASN007 in preclinical cancer models.
  • To explore the combination therapy of ASN007 with PI3K inhibitors.

Main Methods:

  • Preclinical studies using cancer cell lines and tumor models.
  • Assessment of antiproliferative activity of ASN007.
  • Evaluation of combination therapy with PI3K inhibitor copanlisib in vitro and in vivo.

Main Results:

  • ASN007 demonstrated significant antiproliferative activity against tumors with BRAF and RAS mutations.
  • ASN007 showed efficacy in a BRAFV600E melanoma model resistant to BRAF and MEK inhibitors.
  • Combination of ASN007 with copanlisib enhanced antitumor activity through dual pathway inhibition.

Conclusions:

  • ASN007 is a promising therapeutic agent for RAS/RAF-driven cancers.
  • Dual inhibition of RAS/MAPK and PI3K pathways offers a rational combination strategy.
  • Further clinical evaluation of ASN007, particularly in combination therapy, is warranted.
Keywords:
ASN007ERKKRASPI3KRAF/RAS-driven cancersbiomarkercombinational therapykinase inhibitorlymphomasolid tumors

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