Publication

Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines.

Authors not recorded

Leuk Res2008PMID 18191450stubpubmedPublished

Abstract

Abstract (excerpt)

Only the opening of the abstract is shown; abstract text may carry publisher copyright.

Data not yet available

No abstract stored. Read on PubMed

Linked entities

Linked entities (22)

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 22

cancerChronic Myeloid Leukemia, BCR-ABL1 Positivecivic_curation1.00
cancerMalignant Neoplasmcivic_curation1.00
drugBafetinibcivic_curation1.00
drugDasatinibcivic_curation1.00
drugImatinibcivic_curation1.00
drugNilotinibcivic_curation1.00
geneABCB1civic_curation1.00
geneABL1civic_curation1.00
geneLYNcivic_curation1.00
variantABCB1 Overexpressioncivic_curation1.00
variantABL1 F317Lcivic_curation1.00
variantABL1 F317Vcivic_curation1.00
variantABL1 Fusioncivic_curation1.00
variantABL1 G250Ecivic_curation1.00
variantABL1 H396Pcivic_curation1.00
variantABL1 M244Vcivic_curation1.00
variantABL1 M351Tcivic_curation1.00
variantABL1 Q252Hcivic_curation1.00
variantABL1 T315Acivic_curation1.00
variantABL1 T315Icivic_curation1.00
variantABL1 Y253Fcivic_curation1.00
variantLYN OVEREXPRESSIONcivic_curation1.00

Curated evidence

Evidence citing this paper (26)

civicCuratedShowing 1–26 of 26 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
ABCB1 Overexpression1
Bafetinib + DasatinibSubstitutes	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	3	accepted	EID2681 The BCR-ABL1 expressing imatinib-resistant cell line K562/D1-9 overexpresses P-glycoprotein (ABCB1), a known drug membrane transporter. Bafetinib (INNO-406) and dasatinib showed drastically higher IC5… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 Fusion1
Bafetinib + Dasatinib + NilotinibSubstitutes	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID7838 In an in vitro study, six CML cell lines expressing the BCR-ABL1 fusion protein showed sensitivity to nilotinib (IC50: 24.3-84.5 nM), dasatinib (IC50: 1.5-10.9 nM), and bafetinib (IC50: 11.8-87.7 nM).… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
LYN OVEREXPRESSION3
Bafetinib + DasatinibSubstitutes	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID7874 The BCR-ABL1 expressing imatinib-resistant cell line MYL-R overexpresses LYN, an SRC family kinase. Dasatinib showed the most potency against MYL-R compared to the non-resistant MYL cell line (IC50: 6… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Nilotinib	Chronic Myeloid Leukemia, BCR-ABL1 PositiveALIAS	Predictive	D	Supports Resistance	1	accepted	EID7875 The BCR-ABL1 expressing imatinib-resistant cell line MYL-R overexpresses LYN, an SRC family kinase. Nilotinib showed 3.1 times less potency than bafetinib (INNO-406) against MYL-R (IC50: 993.6 nM vs. … (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Dasatinib	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	rejected	EID9085 The BCR-ABL1 expressing imatinib-resistant cell line MYL-R overexpresses LYN, an SRC family kinase. Dasatinib exhibited similar potency against MYL-R (IC50: 6.4 nM) as compared to MYL cell lines (IC50… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 F317L + ABL1 Fusion2
Dasatinib + ImatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7839 In an in vitro study, a Ba/F3 cell line stably expressing the F317L mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib and dasatinib treatment (IC50… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID2677 In an in vitro study, a Ba/F3 cell line stably expressing the F317L mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to nilotinib and bafetinib treat… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 F317V + ABL1 Fusion2
Dasatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7845 In an in vitro study, a Ba/F3 cell line stably expressing F317V in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to dasatinib treatment (IC50: >2000.0 nM) as compared … (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + Imatinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID7843 In an in vitro study, a Ba/F3 cell line stably expressing the dasatinib-resistance variant F317V in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to imatinib,… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 G250E + ABL1 Fusion3
Dasatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID9083 In an in vitro study, a Ba/F3 cell line stably expressing the G250E mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with increased sensitivity to dasatinib treatment (IC50: … (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + ImatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7853 In an in vitro study, a Ba/F3 cell line stably expressing the G250E mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib and bafetinib (INNO-406) trea… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Nilotinib	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID2649 In an in vitro study, a Ba/F3 cell line stably expressing the G250E mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to nilotinib treatment (IC50: 86… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 H396P + ABL1 Fusion3
Dasatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID9084 In an in vitro study, a Ba/F3 cell line stably expressing H396P in the ABL1 portion of the BCR-ABL1 fusion protein was associated with increased sensitivity to dasatinib treatment (IC50: 8.9 nM) as co… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Imatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7847 In an in vitro study, a Ba/F3 cell line stably expressing H396P in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib treatment (IC50: >2000.0 nM) as compared t… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID7846 In an in vitro study, a Ba/F3 cell line stably expressing H396P in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to nilotinib and bafetinib (INNO-406) treatme… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 M244V + ABL1 Fusion2
Bafetinib + ImatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7850 In an in vitro study, a Ba/F3 cell line stably expressing the M244V mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib and bafetinib (INNO-406) trea… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Dasatinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID2640 In an in vitro study, a Ba/F3 cell line stably expressing the M244V mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to dasatinib and nilotinib treat… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 M351T + ABL1 Fusion2
Imatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7841 In an in vitro study, a Ba/F3 cell line stably expressing the M351T mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib treatment (IC50: >2000.0 nM) … (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + Dasatinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID2686 In an in vitro study, a Ba/F3 cell line stably expressing the M351T mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to nilotinib, dasatinib, and baf… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 Q252H + ABL1 Fusion2
Bafetinib + ImatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7849 In an in vitro study, a Ba/F3 cell line stably expressing the Q252H mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib and bafetinib (INNO-406) trea… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Dasatinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID2653 In an in vitro study, a Ba/F3 cell line stably expressing the Q252H mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to dasatinib and nilotinib treat… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 T315A + ABL1 Fusion2
Dasatinib + ImatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7844 In an in vitro study, a Ba/F3 cell line stably expressing T315A in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib and dasatinib treatment (IC50: >2000.0 nM)… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID7842 In an in vitro study, a Ba/F3 cell line stably expressing the dasatinib-resistance variant T315A in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to nilotinib… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 T315I + ABL1 Fusion1
Bafetinib + Dasatinib + Imatinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID2671 In an in vitro study, a Ba/F3 cell line stably expressing the T315I mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to nilotinib, imatinib, dasatinib, and ba… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
ABL1 Y253F + ABL1 Fusion2
Imatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	3	accepted	EID7848 In an in vitro study, a Ba/F3 cell line stably expressing the Y253F mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with resistance to imatinib treatment (IC50: > 2000.0 nM)… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic
Bafetinib + Dasatinib + NilotinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Resistance	3	accepted	EID2658 In an in vitro study, a Ba/F3 cell line stably expressing the Y253F mutation in the ABL1 portion of the BCR-ABL1 fusion protein was associated with similar sensitivity to nilotinib, dasatinib, and baf… (full text at CIViC) PMID 18191450 · Deguchi et al., 2008 · Open in CIViC	civic