Repositioning Candidate Details
| Candidate ID: | R0368 |
| Source ID: | DB01254 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Dasatinib |
| Synonyms: | |
| Molecular Formula: | C22H26ClN7O2S |
| SMILES: | CC1=NC(NC2=NC=C(S2)C(=O)NC2=C(C)C=CC=C2Cl)=CC(=N1)N1CCN(CCO)CC1 |
| Structure: |
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| DrugBank Description: | Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR. |
| CAS Number: | 302962-49-8 |
| Molecular Weight: | 488.006 |
| DrugBank Indication: | 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. |
| DrugBank Pharmacology: | Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor |
| DrugBank MoA: | 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. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression. |
| Targets: | Tyrosine-protein kinase ABL1; Proto-oncogene tyrosine-protein kinase Src; Ephrin type-A receptor 2; Tyrosine-protein kinase Lck; Tyrosine-protein kinase Yes; Mast/stem cell growth factor receptor Kit; Platelet-derived growth factor receptor beta; Signal transducer and activator of transcription 5B; Abelson tyrosine-protein kinase 2; Tyrosine-protein kinase Fyn; Tyrosine-protein kinase BTK; Nuclear receptor subfamily 4 group A member 3; Breakpoint cluster region protein; Tyrosine-protein kinase CSK; Ephrin type-A receptor 5; Ephrin type-B receptor 4; Tyrosine-protein kinase Fgr; Tyrosine-protein kinase FRK; Heat shock cognate 71 kDa protein; Tyrosine-protein kinase Lyn; Mitogen-activated protein kinase kinase kinase MLT; Mitogen-activated protein kinase 14; Amidophosphoribosyltransferase |
| Inclusion Criteria: |
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