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US Approved Rx

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Primary Target

Ephrin type-A receptor 2

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Platelet-derived growth factor receptor beta

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SRC

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Tyrosine-protein kinase ABL

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DASATINIB ANHYDROUS

X78UG0A0RN

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Status:

US Approved Rx (2006)

First approved in 2006

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Platelet-derived growth factor receptor beta

Stem cell growth factor receptor

Ephrin type-A receptor 2

Tyrosine-protein kinase ABL

Conditions:

Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML)

Acute lymphoblastic leukemia

Dasatinib [BMS 354825] is an orally active, small molecule, dual inhibitor of both SRC and ABL kinases that is under development with Bristol-Myers Squibb for the treatment of patients with chronic myelogenous leukaemia (CML) and imatinib-acquired re...

sistance/intolerance. It’s used for the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy. While imatinib remains a frontline therapy for CML, patients with advanced disease frequently develop resistance to imatinib therapy through multiple mechanisms. Dasatinib is also undergoing preclinical evaluation for its potential as a therapy against multiple myeloma. Bristol-Myers Squibb has a composition-of-matter patent covering this research approach that will expire in 2020. Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase.

Dasatinib Laurylsulfate

FY77PS0C4O

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Search for Structure

Status:

US Approved Rx (2006)

First approved in 2006

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Platelet-derived growth factor receptor beta

Stem cell growth factor receptor

Ephrin type-A receptor 2

Tyrosine-protein kinase ABL

Conditions:

Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML)

Acute lymphoblastic leukemia

Dasatinib [BMS 354825] is an orally active, small molecule, dual inhibitor of both SRC and ABL kinases that is under development with Bristol-Myers Squibb for the treatment of patients with chronic myelogenous leukaemia (CML) and imatinib-acquired re...

sistance/intolerance. It’s used for the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy. While imatinib remains a frontline therapy for CML, patients with advanced disease frequently develop resistance to imatinib therapy through multiple mechanisms. Dasatinib is also undergoing preclinical evaluation for its potential as a therapy against multiple myeloma. Bristol-Myers Squibb has a composition-of-matter patent covering this research approach that will expire in 2020. Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase.

DASATINIB

RBZ1571X5H

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Search for Structure

Status:

US Approved Rx (2006)

First approved in 2006

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Platelet-derived growth factor receptor beta

Stem cell growth factor receptor

Ephrin type-A receptor 2

Tyrosine-protein kinase ABL

Conditions:

Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML)

Acute lymphoblastic leukemia

Dasatinib [BMS 354825] is an orally active, small molecule, dual inhibitor of both SRC and ABL kinases that is under development with Bristol-Myers Squibb for the treatment of patients with chronic myelogenous leukaemia (CML) and imatinib-acquired re...

sistance/intolerance. It’s used for the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy. While imatinib remains a frontline therapy for CML, patients with advanced disease frequently develop resistance to imatinib therapy through multiple mechanisms. Dasatinib is also undergoing preclinical evaluation for its potential as a therapy against multiple myeloma. Bristol-Myers Squibb has a composition-of-matter patent covering this research approach that will expire in 2020. Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase.

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