The Multi-Kinase Inhibitor EC-70124 Is a Promising Candidate for the Treatment of FLT3-ITD-Positive Acute Myeloid Leukemia

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López Millán, Belén and Costales, Paula and Gutiérrez Agüera, Francisco and Díaz de la Guardia, Rafael and Roca Ho, Heleia and Vinyoles, Meritxell and Rubio Gayarre, Alba and Safi, Rémi and Castaño, Julio and Romecín, Paola Alejandra and Ramirez Orellana, Manuel and Anguita Mandly, Eduardo and Jeremías, Irmela and Zamora, Lurdes and Rodríguez Manzaneque, Juan Carlos and Bueno, Clara and Morís, Francisco and Menéndez, Pablo (2022) The Multi-Kinase Inhibitor EC-70124 Is a Promising Candidate for the Treatment of FLT3-ITD-Positive Acute Myeloid Leukemia. Cancers, 14 (6). p. 1593. ISSN 2072-6694

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Official URL: https://doi.org/10.3390/cancers14061593




Abstract

Patients with AML harboring constitutively active mutations in the FLT3 receptor generally have a poor prognosis (FLT3-ITDMUT). Despite the fact that several FLT3 inhibitors have been developed, clinical responses are commonly partial or not durable, highlighting the need for new molecules targeting FLT3-ITDMUT. Here, we tested EC-70124, a hybrid indolocarbazole analog from the same chemical space as midostaurin (a well-known FLT3 inhibitor). Our in vitro and in vivo experiments showed that EC-70124 exerts a robust and specific antileukemia activity against FLT3-ITDMUT AML cells while sparing healthy hematopoietic cells. Collectively, EC-70124 is a promising and safe agent for the treatment of this aggressive type of AML.


Item Type:Article
Uncontrolled Keywords:AML; EC-70124 multi-kinase inhibitor; FLT3-ITD mutation; FLT3 inhibitor; AML preclinical model
Subjects:Medical sciences > Medicine > Oncology
ID Code:72851
Deposited On:17 Jun 2022 15:47
Last Modified:27 Jun 2022 08:52

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