^
Association details:
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Source:
Title:

In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants

Excerpt:
...which shows a model of AMN107 in complex with Abl kinase mutant M351T, and shows that the sensitivity of Bcr-Abl mutants to AMN107 segregates into four categories: high (IC50 ≤ 70 nmol/L: M244V, G250E, Q252H, F3llL, F317L, M351T, V379I, L387M, H396P, H396R), medium (IC50 ≤ 200 nmol/L: Y253F, E255K, F359V), low (IC50 ≤ 450 nmol/L: Y253H, E255V), and insensitive (IC50 > 2 μmol/L: T315I).
DOI:
10.1158/0008-5472.CAN-05-0259