Drug intelligence / Profile preview

EC-70124

Development stage
Unknown
Lead developer
AI Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

EC-70124 is a **novel, orally bioavailable, multi-kinase inhibitor** derived from the indolocarbazole chemical space, structurally related to midostaurin but with a more focused kinase inhibition profile. It is designed to inhibit several critical oncogenic kinases, notably **FLT3 (FMS-like tyrosine kinase 3)** including FLT3-ITD mutants, **PIM kinases**, and other kinases involved in tumor proliferation and survival, such as those in the PI3K/AKT/mTOR, JAK/STAT, and NF-κB pathways. EC-70124 has demonstrated selective and potent activity in preclinical models of acute myeloid leukemia (AML), especially FLT3-ITD mutant AML, as well as efficacy in various solid tumor models including sarcoma, glioblastoma, prostate, colorectal, and breast cancer. EC-70124 induces cell cycle arrest and apoptosis, blocks key signaling nodes (pSTAT5, pBAD, mTOR-S6, p4EBP1, pAKT, pSTAT3, IKKβ/NF-κB), inhibits cancer stem cell properties, and is able to reverse drug resistance mediated by ABC transporters. The developer is EntreChem, with AML as the lead indication in clinical development[1][2][3][4][5][11].

02

Targets

PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)mTOR (Mammalian target of rapamycin kinase)FLT3 (Fms related receptor tyrosine kinase 3)PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)JAK2 (Janus kinase 2)PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)SYK (Spleen Tyrosine Kinase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)

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