Novel dual Src/Abl inhibitors for hematologic and solid malignancies

Phase 1 pharmacokinetic and drug-interaction study of dasatinib in patients with advanced solid tumors

(2010) Faye M. Johnson et al.   CANCER

New Opportunities to Treat the T315I-Bcr-Abl Mutant in Chronic Myeloid Leukaemia: Tyrosine Kinase Inhibitors and Molecules that Act by Alternative Mechanisms

(2010) S. Schenone et al.   CURRENT MEDICINAL CHEMISTRY

Phase I/II Study of the Src Inhibitor Dasatinib in Combination With Erlotinib in Advanced Non–Small-Cell Lung Cancer

(2010) Eric B. Haura et al.   JOURNAL OF CLINICAL ONCOLOGY

A Phase II Study of Dasatinib in Patients with Chemosensitive Relapsed Small Cell Lung Cancer (Cancer and Leukemia Group B 30602)

(2010) Antonius A. Miller et al.   Journal of Thoracic Oncology

A Bead-Based Activity Screen for Small-Molecule Inhibitors of Signal Transduction in Chronic Myelogenous Leukemia Cells

(2010) J. E. Sylvester et al.   MOLECULAR CANCER THERAPEUTICS

A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study

(2009) Primo N. Lara et al.   ANTI-CANCER DRUGS

Network analyses in systems pharmacology

(2009) S. I. Berger et al.   BIOINFORMATICS

Dasatinib treatment of chronic-phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations

(2009) M. C. Muller et al.   BLOOD

Philadelphia-positive patients who already harbor imatinib-resistant Bcr-Abl kinase domain mutations have a higher likelihood of developing additional mutations associated with resistance to second- or third-line tyrosine kinase inhibitors

(2009) S. Soverini et al.   BLOOD

BCR-ABL promotes the frequency of mutagenic single-strand annealing DNA repair

(2009) M. S. Fernandes et al.   BLOOD

Phase 3 study of dasatinib 140 mg once daily versus 70 mg twice daily in patients with chronic myeloid leukemia in accelerated phase resistant or intolerant to imatinib: 15-month median follow-up

(2009) H. Kantarjian et al.   BLOOD

The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines

(2009) Patricia Mambou Gwanmesia et al.   BMC CANCER

Dasatinib inhibits the growth of prostate cancer in bone and provides additional protection from osteolysis

(2009) T Koreckij et al.   BRITISH JOURNAL OF CANCER

Dasatinib synergizes with doxorubicin to block growth, migration and invasion of breast cancer cells

(2009) C S Pichot et al.   BRITISH JOURNAL OF CANCER

Dasatinib treatment for Philadelphia chromosome-positive leukemias

(2009) Hanna Jean Khoury et al.   CANCER

Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia resistant to imatinib at a dose of 400 to 600 milligrams daily

(2009) Hagop Kantarjian et al.   CANCER

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

Synergistic Activity of the Src Family Kinase Inhibitor Dasatinib and Oxaliplatin in Colon Carcinoma Cells Is Mediated by Oxidative Stress

(2009) S. Kopetz et al.   CANCER RESEARCH

Effects of Src inhibitors on cell growth and epidermal growth factor receptor and MET signaling in gefitinib-resistant non-small cell lung cancer cells with acquired MET amplification

(2009) Takeshi Yoshida et al.   CANCER SCIENCE

SRC kinase inhibition: Targeting bone metastases and tumor growth in prostate and breast cancer

(2009) Fred Saad et al.   CANCER TREATMENT REVIEWS

AP24163 Inhibits the Gatekeeper Mutant of BCR-ABL and SuppressesIn vitroResistance

(2009) Mohammad Azam et al.   Chemical Biology & Drug Design

Phase II Study of Dasatinib in Patients with Metastatic Castration-Resistant Prostate Cancer

(2009) E. Y. Yu et al.   CLINICAL CANCER RESEARCH

Phase I Dose-Escalation and Pharmacokinetic Study of Dasatinib in Patients with Advanced Solid Tumors

(2009) G. D. Demetri et al.   CLINICAL CANCER RESEARCH

Combined Src and Aromatase Inhibition Impairs Human Breast Cancer Growth In vivo and Bypass Pathways Are Activated in AZD0530-Resistant Tumors

(2009) Y. Chen et al.   CLINICAL CANCER RESEARCH

Reciprocal Regulation of c-Src and STAT3 in Non-Small Cell Lung Cancer

(2009) L. A. Byers et al.   CLINICAL CANCER RESEARCH

Antitumor Effects and Biomarkers of Activity of AZD0530, a Src Inhibitor, in Pancreatic Cancer

(2009) N.V. Rajeshkumar et al.   CLINICAL CANCER RESEARCH

New approved dasatinib regimen available for clinical use

(2009) David S Snyder   Expert Review of Anticancer Therapy

Activity of tyrosine kinase inhibitor Dasatinib in neuroblastoma cellsin vitroand in orthotopic mouse model

(2009) Roberta Vitali et al.   INTERNATIONAL JOURNAL OF CANCER

Effects of the Src kinase inhibitor saracatinib (AZD0530) on bone turnover in healthy men: A randomized, double-blind, placebo-controlled, multiple-ascending-dose phase I trial

(2009) Rosemary A Hannon et al.   JOURNAL OF BONE AND MINERAL RESEARCH

9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation

(2009) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Improving the prognosis for patients with glioblastoma: the rationale for targeting Src

(2009) John de Groot et al.   JOURNAL OF NEURO-ONCOLOGY

P-glycoprotein and Breast Cancer Resistance Protein Influence Brain Distribution of Dasatinib

(2009) Y. Chen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Therapeutic implications of Src independent calcium mobilization in diffuse large B-cell lymphoma

(2009) C. Annette Hollmann et al.   LEUKEMIA RESEARCH

Src activation in melanoma and Src inhibitors as therapeutic agents in melanoma

(2009) Jade Homsi et al.   MELANOMA RESEARCH

Dasatinib-induced autophagy is enhanced in combination with temozolomide in glioma

(2009) V. Milano et al.   MOLECULAR CANCER THERAPEUTICS

Efficacy and pharmacodynamic effects of bosutinib (SKI-606), a Src/Abl inhibitor, in freshly generated human pancreas cancer xenografts

(2009) W. A. Messersmith et al.   MOLECULAR CANCER THERAPEUTICS

Effects of Src kinase inhibition induced by dasatinib in non-small cell lung cancer cell lines treated with cisplatin

(2009) P. Ceppi et al.   MOLECULAR CANCER THERAPEUTICS

Activity of dasatinib against L576P KIT mutant melanoma: Molecular, cellular, and clinical correlates

(2009) S. E. Woodman et al.   MOLECULAR CANCER THERAPEUTICS

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530

(2009) Tim P. Green et al.   Molecular Oncology

Target profiling of small molecules by chemical proteomics

(2009) Uwe Rix et al.   Nature Chemical Biology

Imatinib and beyond—exploring the full potential of targeted therapy for CML

(2009) Alfonso Quintás-Cardama et al.   Nature Reviews Clinical Oncology

Treatment selection after imatinib resistance in chronic myeloid leukemia

(2009) Elias Jabbour et al.   Targeted Oncology

Predicting drug side-effects by chemical systems biology

(2009) Nicholas P Tatonetti et al.   GENOME BIOLOGY

Targeting Src in breast cancer

(2008) R. S. Finn   ANNALS OF ONCOLOGY

Src as a therapeutic target in men with prostate cancer and bone metastases

(2008) Fred Saad   BJU INTERNATIONAL

Molecular biology of bcr-abl1-positive chronic myeloid leukemia

(2008) A. Quintas-Cardama et al.   BLOOD

Dasatinib crosses the blood-brain barrier and is an efficient therapy for central nervous system Philadelphia chromosome-positive leukemia

(2008) K. Porkka et al.   BLOOD

Dual targeting of Src and ER prevents acquired antihormone resistance in breast cancer cells

(2008) S. Hiscox et al.   BREAST CANCER RESEARCH AND TREATMENT

Effects of dasatinib on EphA2 receptor tyrosine kinase activity and downstream signalling in pancreatic cancer

(2008) Q Chang et al.   BRITISH JOURNAL OF CANCER

Effects of Dasatinib on Src Kinase Activity and Downstream Intracellular Signaling in Primitive Chronic Myelogenous Leukemia Hematopoietic Cells

(2008) H. Konig et al.   CANCER RESEARCH

Targeting Src Family Kinases Inhibits Growth and Lymph Node Metastases of Prostate Cancer in an Orthotopic Nude Mouse Model

(2008) S. I. Park et al.   CANCER RESEARCH

Aberrant Activation of Androgen Receptor in a New Neuropeptide-Autocrine Model of Androgen-Insensitive Prostate Cancer

(2008) J. C. Yang et al.   CANCER RESEARCH

New developments in multitargeted therapy for patients with solid tumours

(2008) C. Le Tourneau et al.   CANCER TREATMENT REVIEWS

C6-Unsubstituted Pyrazolo[3,4-d]pyrimidines Are Dual Src/Abl Inhibitors Effective against Imatinib Mesylate Resistant Chronic Myeloid Leukemia Cell Lines

(2008) Maria Alessandra Santucci et al.   ChemMedChem

Expression of Src and FAK in Hepatocellular Carcinoma and the Effect of Src Inhibitors on Hepatocellular Carcinoma In Vitro

(2008) Grace M. Lau et al.   DIGESTIVE DISEASES AND SCIENCES

Cytotoxic effects of a novel pyrazolopyrimidine derivative entrapped in liposomes in anaplastic thyroid cancer cells in vitro and in xenograft tumors in vivo

(2008) M Celano et al.   ENDOCRINE-RELATED CANCER

Antiproliferative and proapoptotic activities of new pyrazolo[3,4-d]pyrimidine derivative Src kinase inhibitors in human osteosarcoma cells

(2008) Adriano Spreafico et al.   FASEB JOURNAL

Activation of Src and Src-associated signaling pathways in relation to hypoxia in human cancer xenograft models

(2008) Nhu-An Pham et al.   INTERNATIONAL JOURNAL OF CANCER

Preclinical evaluation of dasatinib, a potent Src kinase inhibitor, in melanoma cell lines

(2008) Alex J Eustace et al.   Journal of Translational Medicine

Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells

(2008) L L Remsing Rix et al.   LEUKEMIA

Tyrosine kinase inhibition in diffuse large B-cell lymphoma: molecular basis for antitumor activity and drug resistance of dasatinib

(2008) C Yang et al.   LEUKEMIA

Efficacy and safety of dasatinib in imatinib-resistant or -intolerant patients with chronic myeloid leukemia in blast phase

(2008) J Cortes et al.   LEUKEMIA

Inhibition of Src Family Kinases with Dasatinib Blocks Migration and Invasion of Human Melanoma Cells

(2008) R. Buettner et al.   MOLECULAR CANCER RESEARCH

SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells

(2008) A. Vultur et al.   MOLECULAR CANCER THERAPEUTICS

Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy

(2008) Jinyan Du et al.   NATURE BIOTECHNOLOGY

Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530

(2008) Y-M Chang et al.   ONCOGENE