Publication

In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.

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Cancer Res2005PMID 15930265stubpubmedPublished

Abstract

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Linked entities

Linked entities (14)

How each link was made (MeSH, dictionary, registry reference, curation…) and whether it has been validated. Candidate links are not counted in entity statistics.

Validated 14

cancerChronic Myeloid Leukemia, BCR-ABL1 Positivecivic_curation1.00
cancerMalignant Neoplasmcivic_curation1.00
drugImatinibcivic_curation1.00
geneABL1civic_curation1.00
variantABL1 E255Kcivic_curation1.00
variantABL1 F317Lcivic_curation1.00
variantABL1 F359Vcivic_curation1.00
variantABL1 Fusioncivic_curation1.00
variantABL1 G250Ecivic_curation1.00
variantABL1 H396Rcivic_curation1.00
variantABL1 M244Vcivic_curation1.00
variantABL1 M351Tcivic_curation1.00
variantABL1 T315Icivic_curation1.00
variantABL1 Y253Fcivic_curation1.00

Curated evidence

Evidence citing this paper (27)

civicCuratedShowing 1–27 of 27 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
ABL1 BCR::ABL D276G1
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	C	Supports Resistance	—	rejected	EID2665 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 BCR::ABL L248V1
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	C	Supports Resistance	—	rejected	EID2643 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 E255K + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4349 In an in vitro study, a Ba/F3 cell line expressing an E255K mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (5.6 nmol/L vs. 0.8 nmol/… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	3	accepted	EID2661 A panel of 16 mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations were compared with non-mutated BCR-ABL protein and evaluated for anti-prolif… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 E255V + ABL1 Fusion1
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4450 In an in vitro study, a Ba/F3 cell line expressing an E255V mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (11.0 nmol/L vs. 0.8 nmol… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 F311L + ABL1 Fusion1
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4548 In an in vitro study, a Ba/F3 cell line expressing a F311L mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (1.3 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 F317L + ABL1 Fusion2
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID2676 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
〃	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID2680 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 F359V + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID3821 In an in vitro study, a Ba/F3 cell line expressing a F359V mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (2.2 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	C	Supports Resistance	2	accepted	EID2169 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 G250E + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4315 In an in vitro study, a Ba/F3 cell line expressing a G250E mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (IC50: 1.8 nmol/L vs. 0.8 … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID2647 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 H396P + ABL1 Fusion1
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4558 In an in vitro study, a Ba/F3 cell line expressing a H396P mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (0.6 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 H396R + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4412 In an in vitro study, a Ba/F3 cell line expressing a H396R mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (1.3 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	accepted	EID2689 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 L387M + ABL1 Fusion1
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4408 In an in vitro study, a Ba/F3 cell line expressing a L387M mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (2.0 nmol/L vs. 0.8 nmol/… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 M244V + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4306 In an in vitro study, a Ba/F3 cell line expressing an M244V mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (IC50: 1.3 nmol/L vs. 0.8… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID2638 A panel of 16 mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations were compared with non-mutated BCR-ABL protein and evaluated for antiprolife… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 M351T + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4395 In an in vitro study, a Ba/F3 cell line expressing an M351T mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (1.1 nmol/L vs. 0.8 nmol/… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID2684 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 Q252H + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	2	submitted	EID4322 In an in vitro study, a Ba/F3 cell line expressing a Q252H mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (3.4 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	C	Supports Sensitivity Response	2	submitted	EID2652 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 T315I + ABL1 Fusion1
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	4	accepted	EID2669 A panel of 16 mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations were compared with non-mutated BCR-ABL protein and evaluated for anti-prolif… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 V379I + ABL1 Fusion1
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	1	submitted	EID4705 In an in vitro study, a Ba/F3 cell line expressing a V379I mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (0.8 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 Y253F + ABL1 Fusion2
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID4342 In an in vitro study, a Ba/F3 cell line expressing a Y253F mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (1.4 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
Imatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	3	accepted	EID2657 In two cell-based studies, a panel of either 18 or 16 mutations representing 85% of known mutations seen in imatinib CML patents were used to evaluate the effectiveness of drug binding. All mutations … (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic
ABL1 Y253H + ABL1 Fusion1
Dasatinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	2	submitted	EID4338 In an in vitro study, a Ba/F3 cell line expressing a Y253H mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with sensitivity to dasatinib treatment (1.3 nmol/L vs. 0.8 nmol/L… (full text at CIViC) PMID 15930265 · O'Hare et al., 2005 · Open in CIViC	civic