1. Protein Tyrosine Kinase/RTK
  2. Src
    Bcr-Abl

Bosutinib (Synonyms: SKI-606)

Cat. No.: HY-10158 Purity: 99.83%
Data Sheet SDS Handling Instructions

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively.

For research use only. We do not sell to patients.
Bosutinib Chemical Structure

Bosutinib Chemical Structure

CAS No. : 380843-75-4

Size Price Stock Quantity
1 mg   Get quote  
5 mg   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively. IC50 value: 1.2 nM/1 nM (Src/Abl) [1] Target: Src/Abl in vitro: Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM [1]. Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation [2]. Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin [3]. in vivo: Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively [1]. Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity [2]. As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts [4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02906696 M.D. Anderson Cancer Center|Pfizer Chronic Myelogenous Leukemia October 2016 Phase 2
NCT01331291 Massachusetts General Hospital|Dana-Farber Cancer Institute|Brigham and Women's Hospital|Pfizer Glioblastoma April 2011 Phase 2
NCT02311998 M.D. Anderson Cancer Center|Pfizer Leukemia April 2015 Phase 1|Phase 2
NCT02810990 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Myeloid Leukemia November 2016 Phase 2
NCT03023319 Nagla Karim|University of Cincinnati Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer January 2017 Phase 1
NCT02782403 M.D. Anderson Cancer Center|Pfizer Leukemia March 20, 2017 Phase 1|Phase 2
NCT03128411 Pfizer Leukemia, Chronic Myelogenous May 15, 2017 Phase 2
NCT02445742 PETHEMA Foundation Chronic Myeloblastic Leukaemia May 2015 Phase 2
NCT02130557 Avillion Development 1 Limited Leukemia, Myelogenous, Chronic, Breakpoint Cluster Region-Abelson Proto-oncogene (BCR-ABL) Positive June 2014 Phase 3
NCT01374139 Pfizer Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) August 2011 Phase 1
NCT02546375 Pfizer|pH Associates Chronic Myeloid Leukaemia July 2015
NCT01903733 Pfizer Chronic Myeloid Leukemia August 28, 2013
NCT01025570 University of California, San Francisco|University of Utah Pancreatic Cancer May 2010 Phase 1
NCT00261846 Pfizer Chronic Myeloid Leukemia March 2006 Phase 1|Phase 2
NCT00574873 Pfizer|Wyeth is now a wholly owned subsidiary of Pfizer Chronic Myeloid Leukemia February 2008 Phase 3
NCT02192294 Pfizer Healthy August 2014 Phase 1
NCT00934674 Wyeth is now a wholly owned subsidiary of Pfizer Healthy July 2009 Phase 1
NCT00959946 Pfizer Advanced Breast Cancer (Parts 1 and 2)|Advanced Pancreatic Cancer (Part 1)|Advanced Colorectal Cancer (Part 1)|Advanced Cholangiocarcinoma (Part 1)|Advanced Glioblastoma Multiforme (Part 1) September 2009 Phase 1|Phase 2
NCT00721474 Wyeth is now a wholly owned subsidiary of Pfizer Healthy Subjects September 2008 Phase 1
NCT01080365 Wyeth is now a wholly owned subsidiary of Pfizer Healthy February 2010 Phase 1
NCT02058277 Pfizer Healthy May 2014 Phase 1
NCT01233869 Pfizer Polycystic Kidney, Autosomal Dominant December 2010 Phase 2
NCT02102633 Pfizer Healthy May 2014 Phase 1
NCT00952913 Wyeth is now a wholly owned subsidiary of Pfizer Healthy August 2009 Phase 1
NCT00725426 Wyeth is now a wholly owned subsidiary of Pfizer Healthy July 2008 Phase 1
NCT00811070 Pfizer Chronic Myelogenous Leukemia December 2007 Phase 2
NCT02501330 Pfizer Chronic Myelogenous Leukemia July 1, 2015
NCT03106779 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia August 15, 2017 Phase 3
NCT01233882 Pfizer Renal Disease, End-Stage|Renal Insufficiency, Chronic|Renal Insufficiency, Acute December 2010 Phase 1
NCT00793546 Pfizer Advanced Breast Cancer February 2009 Phase 2
NCT02228382 Pfizer|Developmental Therapeutics Consortium Previously Treated PH + CML November 7, 2014 Phase 4
NCT00319254 Pfizer Breast Neoplasms|Neoplasm Metastasis May 2006 Phase 2
NCT00759837 Wyeth is now a wholly owned subsidiary of Pfizer Breast Cancer|Leukemia, Myeloid, Chronic October 2008 Phase 1
NCT00880009 Pfizer Breast Cancer July 2009 Phase 2
NCT00777530 Wyeth is now a wholly owned subsidiary of Pfizer Breast Cancer|Tumors|Leukemia April 2008 Phase 1
NCT00195260 Pfizer Neoplasms October 2004 Phase 1
NCT02638467 University of Milano Bicocca|IRCCS San Raffaele Leukemia|Myelogenous|Chronic|BCR-ABL Positive November 2015 Phase 2
NCT02921477 Neurological Associates of West Los Angeles|Pfizer Mild Cognitive Impairment|Dementia September 2016 Phase 1
NCT02693535 American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors March 2016 Phase 2
NCT02906696 M.D. Anderson Cancer Center|Pfizer Chronic Myelogenous Leukemia October 2016 Phase 2
NCT01331291 Massachusetts General Hospital|Dana-Farber Cancer Institute|Brigham and Women's Hospital|Pfizer Glioblastoma April 2011 Phase 2
NCT02311998 M.D. Anderson Cancer Center|Pfizer Leukemia April 2015 Phase 1|Phase 2
NCT02810990 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Myeloid Leukemia November 2016 Phase 2
NCT03023319 Nagla Karim|University of Cincinnati Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer January 2017 Phase 1
NCT02782403 M.D. Anderson Cancer Center|Pfizer Leukemia March 20, 2017 Phase 1|Phase 2
NCT03128411 Pfizer Leukemia, Chronic Myelogenous May 15, 2017 Phase 2
NCT02445742 PETHEMA Foundation Chronic Myeloblastic Leukaemia May 2015 Phase 2
NCT02130557 Avillion Development 1 Limited Leukemia, Myelogenous, Chronic, Breakpoint Cluster Region-Abelson Proto-oncogene (BCR-ABL) Positive June 2014 Phase 3
NCT01374139 Pfizer Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) August 2011 Phase 1
NCT02546375 Pfizer|pH Associates Chronic Myeloid Leukaemia July 2015
NCT01903733 Pfizer Chronic Myeloid Leukemia August 28, 2013
NCT01025570 University of California, San Francisco|University of Utah Pancreatic Cancer May 2010 Phase 1
NCT00261846 Pfizer Chronic Myeloid Leukemia March 2006 Phase 1|Phase 2
NCT00574873 Pfizer|Wyeth is now a wholly owned subsidiary of Pfizer Chronic Myeloid Leukemia February 2008 Phase 3
NCT02192294 Pfizer Healthy August 2014 Phase 1
NCT00934674 Wyeth is now a wholly owned subsidiary of Pfizer Healthy July 2009 Phase 1
NCT00959946 Pfizer Advanced Breast Cancer (Parts 1 and 2)|Advanced Pancreatic Cancer (Part 1)|Advanced Colorectal Cancer (Part 1)|Advanced Cholangiocarcinoma (Part 1)|Advanced Glioblastoma Multiforme (Part 1) September 2009 Phase 1|Phase 2
NCT00721474 Wyeth is now a wholly owned subsidiary of Pfizer Healthy Subjects September 2008 Phase 1
NCT01080365 Wyeth is now a wholly owned subsidiary of Pfizer Healthy February 2010 Phase 1
NCT02058277 Pfizer Healthy May 2014 Phase 1
NCT01233869 Pfizer Polycystic Kidney, Autosomal Dominant December 2010 Phase 2
NCT02102633 Pfizer Healthy May 2014 Phase 1
NCT00952913 Wyeth is now a wholly owned subsidiary of Pfizer Healthy August 2009 Phase 1
NCT00725426 Wyeth is now a wholly owned subsidiary of Pfizer Healthy July 2008 Phase 1
NCT00811070 Pfizer Chronic Myelogenous Leukemia December 2007 Phase 2
NCT02501330 Pfizer Chronic Myelogenous Leukemia July 1, 2015
NCT03106779 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia August 15, 2017 Phase 3
NCT01233882 Pfizer Renal Disease, End-Stage|Renal Insufficiency, Chronic|Renal Insufficiency, Acute December 2010 Phase 1
NCT00793546 Pfizer Advanced Breast Cancer February 2009 Phase 2
NCT02228382 Pfizer|Developmental Therapeutics Consortium Previously Treated PH + CML November 7, 2014 Phase 4
NCT00319254 Pfizer Breast Neoplasms|Neoplasm Metastasis May 2006 Phase 2
NCT00759837 Wyeth is now a wholly owned subsidiary of Pfizer Breast Cancer|Leukemia, Myeloid, Chronic October 2008 Phase 1
NCT00880009 Pfizer Breast Cancer July 2009 Phase 2
NCT00777530 Wyeth is now a wholly owned subsidiary of Pfizer Breast Cancer|Tumors|Leukemia April 2008 Phase 1
NCT00195260 Pfizer Neoplasms October 2004 Phase 1
NCT02638467 University of Milano Bicocca|IRCCS San Raffaele Leukemia|Myelogenous|Chronic|BCR-ABL Positive November 2015 Phase 2
NCT02921477 Neurological Associates of West Los Angeles|Pfizer Mild Cognitive Impairment|Dementia September 2016 Phase 1
NCT02693535 American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors March 2016 Phase 2
NCT01001936 Wyeth is now a wholly owned subsidiary of Pfizer Tumors February 2006 Phase 1
NCT00499538 Wyeth is now a wholly owned subsidiary of Pfizer Healthy July 2007 Phase 1
NCT00406406 Wyeth is now a wholly owned subsidiary of Pfizer Healthy November 2006 Phase 1
NCT00757341 Wyeth is now a wholly owned subsidiary of Pfizer Healthy Subjects December 2008 Phase 1
NCT00434486 Wyeth is now a wholly owned subsidiary of Pfizer Healthy March 2007 Phase 1
NCT00914121 Wyeth is now a wholly owned subsidiary of Pfizer Healthy Subjects June 2009 Phase 1
View MoreCollapse
References
Molecular Weight

530.45

Formula

C₂₆H₂₉Cl₂N₅O₃

CAS No.

380843-75-4

Storage

Powder4°C, protect from light

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 46 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.83%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Bosutinib
Cat. No.:
HY-10158
Quantity: