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Association details:
Evidence:
Evidence Level:
Resistant: D – Preclinical
New
Source:
Title:

Exome sequencing identifies recurring FLT3 N676K mutations in core-binding factor leukemia

Excerpt:
Both compounds potently inhibited FLT3-ITD–expressing cells with a half maximal inhibitory concentration (IC50) of 13 nM for PKC412 and 2.5 nM for AC220, respectively. FLT3 N676K-expressing cells were also sensitive to FLT3 inhibitors with an IC50 of 7.5 nM for PKC412 and 3 nM for AC220. FLT3-ITD-N676K double mutants showed a strong resistance to both inhibitors (IC50 greater than 80 nM for PKC412 and greater than 16 nM for AC220).
DOI:
https://doi.org/10.1182/blood-2013-01-476473