Titles and Legends to Supplementary Tables and Figure

Supplementary Table S1. CML patient sample details. WBC (G/l): white blood count (grams/liter); Hb (g/dl): hemoglobin (grams/deciliter); Plt (G/l): platelets (grams/liter); Basos: basophils; pb: peripheral blood; CRP (mg/dl): c-reactive protein (milligrams/deciliter); HU: hydroxyurea

Supplementary Table S2. All proteins purified on bosutinib matrix from K562 cells. Proteins are sorted by the number of identified unique peptides (peptide counts). IPI-IDs are IPI protein database entries to which identified peptides were assigned. Proteins listed have at least one specific peptide that confirms the presence of the protein in the pull-down. PD1 and PD2 refer to the duplicate pull-downs performed for each cell line.

Supplementary Table S3. All proteins purified on bosutinib matrix from the accelerated phase CML patient 1 cells.Proteins are sorted by the number of identified unique peptides (peptide counts). IPI-IDs are IPI protein database entries to which identified peptides were assigned. Proteins listed have at least one specific peptide that confirms the presence of the protein in the pull-down. PD1 and PD2 refer to the duplicate pull-downs performed for each cell line.

Supplementary Table S4. All proteins purified on bosutinib matrix from the accelerated phase CML patient 2 cells.Proteins are sorted by the number of identified unique peptides (peptide counts). IPI-IDs are IPI protein database entries to which identified peptides were assigned. Proteins listed have at least one specific peptide that confirms the presence of the protein in the pull-down. PD1 and PD2 refer to the duplicate pull-downs performed for each cell line.

Supplementary Table S5. Identified kinase targets of bosutinib. IPI-ID indicates IPI protein database entries to which identified peptides (AvePepCnt) were assigned. Unless otherwise indicated, kinases present in this list have been specifically identified twice in at least one of the three cell types. The average sequence coverage (AveSeqCov) is based on these unique peptides and takes into accountthe size of the protein. If a protein was identified in only one of the two repeats per cell type, then the values are given in italics. Where no peptide was identified to specifically confirm that a protein is present, the values are given in parentheses (x). Proteins are sorted alphabetically. The BCR-ABL fusion protein is split into the componentsBCR and ABL1, plus the short peptide sequence characteristic of the fusion region of BCR-ABL. The top five hits for each cell type are highlighted in bold. PD=Pulldown

Supplementary Table S6. Complete Millipore KinaseProfilerTM panel. For each kinase, the percent activity remaining at 1 µM and 10 µM of bosutinib, c-bosutinib and dasatinib were measured.

Supplementary Table S7.IC50 (nM) or activity (%) remaining at 10 µM determined for selected kinases. Kinases are of human origin unless otherwise stated.

Supplementary Figure Legend

Supplementary Figure S1.Millipore KinaseProfiler Service Assay Protocols. This manual providesthe screening conditionsand protocols used in the MilliporeKinaseProfilerradiometric protein kinase assays and HTRF®lipidkinase assays.

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