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

Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD

Excerpt:
Substitution of the FLT3 “gatekeeper” phenylalanine with leucine (F691L) conferred mild resistance to ponatinib, but substitutions at the FLT3 activation loop (AL) residue D835 conferred a high degree of resistance. Saturation mutagenesis of FLT3-ITD exclusively identified FLT3 AL mutations at positions D835, D839, and Y842....supplemental Figure 1....
DOI:
https://dx.doi.org/10.1182%2Fblood-2012-07-442871