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Association details:
Biomarker:FLT3 F691L
Cancer:Acute Myelogenous Leukemia
Drug:JRF104 (FLT3 inhibitor, AXL inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Source:
Title:

3766 / 20 - Development of new FLT3/AXL dual inhibitor JRF104 with potent FLT3-TKD inhibition

Published date:
05/27/2020
Excerpt:
In vitro studies suggested that JRF104 could potently inhibit the proliferation of MV4-11 and Molm-13 cells, which endogenously express FLT3-ITD mutation. JRF104 shows wide spectrum in vitro antiproliferation activity against all FLT3 mutation types, including the “gate-keeper” F691L mutation. JRF104 can effectively reduce MDA-MB-231 cell migration in vitro, accomplished by blocking tumor migration pathway regulated by AXL...Based on these datas, JRF104 may overcome resistance caused by AXL and FLT3-TKD mutation, representing a novel promising clinical antitumor agent for treating AML patients with FLT3 mutations.