Activity of FB2, a novel dual Abl/Src tyrosine kinase inhibitor, against imatinib-resistant chronic myeloid leukemia in vivo and in vitro.

Abstract:

:FB2 is a novel Abl/Src dual tyrosine kinase inhibitor which is designed to overcome imatinib resistance. Besides imatinib-sensitive cell lines (K562), FB2 significantly inhibited the growth of imatinib-resistant cell lines of different resistance mechanisms (K562/G5.0 and K562/G01), and decreased the expression of autophosphorylation of Bcr/Abl, c-Src and Lyn kinases on them. It also inhibited the proliferation of Src over activated cells DU145 and MDA-MB-231. Furthermore, FB2 potently prolonged the survival time of non-obese diabetic/severe combined immunodeficient mice harboured K562/G5.0 cells. These results indicated that FB2, an Abl/Src dual tyrosine kinase inhibitor, is a promising candidate for imatinib-resistant CML and Src over activated cancer.

journal_name

Leuk Lymphoma

journal_title

Leukemia & lymphoma

authors

Liu H,Li H,Feng Z,Tai J,Meng Y,Wang H,Xin H,Zhang S,Zuo M,Zhang Y,Chen X

doi

10.1080/10428190802709438

subject

Has Abstract

pub_date

2009-03-01 00:00:00

pages

437-46

issue

3

eissn

1042-8194

issn

1029-2403

pii

910217620

journal_volume

50

pub_type

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