| Drug General Information |
| Drug ID |
D0E6XR
|
| Former ID |
DAP000004
|
| Drug Name |
Dasatinib
|
| Synonyms |
Dasatinibum; Sprycel; Spyrcel; Dasatinib [USAN]; Dasatinib anhydrous; BMS 354825; BMS354825; BMS-354825; Dasatinib (USAN); Dasatinib, BMS 354825; SPRYCEL (TN); Sprycel (TN); BMS-354825, Sprycel, BMS354825, Dasatinib; N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide, monohydrate; N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide; N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide; N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide; N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE; (18F)-N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide; 2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide; Tyrosine Kinase Inhibitor - Ns
|
| Drug Type |
Small molecular drug
|
| Indication |
Chronic myelogenous leukaemia [ICD9: 205.1; ICD10:C92.1]
|
Approved |
[1],
[2],
[3],
[4]
|
|---|
|
Multiple myeloma [ICD9: 203; ICD10:C90]
|
Phase 2 |
[5],
[3]
|
| Therapeutic Class |
Anticancer Agents
|
| Company |
Bristol Myers Squibb
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C22H26ClN7O2S
|
| InChI |
InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
|
| InChIKey |
ZBNZXTGUTAYRHI-UHFFFAOYSA-N
|
| CAS Number |
CAS 302962-49-8
|
| PubChem Compound ID |
|
| PubChem Substance ID |
10061134, 12015788, 14859389, 17397755, 17422520, 36127155, 46505143, 46513626, 47883136, 48429642, 49742622, 50070229, 50070567, 50071309, 50100097, 50125840, 52995488, 53799228, 56312240, 56312839, 56313127, 56373968, 56459420, 57288451, 57354110, 57551950, 74374210, 85246174, 87235888, 87357382, 93581026, 99381604, 99437986, 103501621, 103905543, 111644212, 117418208, 117695728, 118050493, 119503515, 124361516, 124756940, 124893650, 124893651, 124893652, 125001912, 125163747, 125264620, 125347447, 126624063
|
| ChEBI ID |
ChEBI:49375
|
| SuperDrug ATC ID |
L01XE06
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Proto-oncogene tyrosine-protein kinase SRC |
Target Info |
Inhibitor |
[6],
[7],
[8]
|
|---|
| Proto-oncogene c-Abl |
Target Info |
Inhibitor |
[6],
[7],
[8]
|
| Lck tyrosine kinase |
Target Info |
Inhibitor |
[6],
[7],
[8]
|
| Fyn tyrosine kinase |
Target Info |
Inhibitor |
[6],
[7],
[8]
|
|
KEGG Pathway
|
ErbB signaling pathway
|
|
Rap1 signaling pathway
|
|
Chemokine signaling pathway
|
|
Endocytosis
|
|
VEGF signaling pathway
|
|
Focal adhesion
|
|
Adherens junction
|
|
Tight junction
|
|
Gap junction
|
|
Platelet activation
|
|
GABAergic synapse
|
|
Inflammatory mediator regulation of TRP channels
|
|
Regulation of actin cytoskeleton
|
|
GnRH signaling pathway
|
|
Estrogen signaling pathway
|
|
Prolactin signaling pathway
|
|
Thyroid hormone signaling pathway
|
|
Oxytocin signaling pathway
|
|
Bacterial invasion of epithelial cells
|
|
Epithelial cell signaling in Helicobacter pylori infection
|
|
Shigellosis
|
|
Tuberculosis
|
|
Hepatitis B
|
|
Viral carcinogenesis
|
|
Proteoglycans in cancerhsa04012:ErbB signaling pathway
|
|
Ras signaling pathway
|
|
Cell cycle
|
|
Axon guidance
|
|
Neurotrophin signaling pathway
|
|
Pathogenic Escherichia coli infection
|
|
Pathways in cancer
|
|
MicroRNAs in cancer
|
|
Chronic myeloid leukemia
|
|
Viral myocarditishsa04064:NF-kappa B signaling pathway
|
|
Osteoclast differentiation
|
|
Natural killer cell mediated cytotoxicity
|
|
T cell receptor signaling pathway
|
|
HTLV-I infection
|
|
Primary immunodeficiencyhsa04071:Sphingolipid signaling pathway
|
|
Fc epsilon RI signaling pathway
|
|
Cholinergic synapse
|
|
Prion diseases
|
|
Measles
|
|
Viral myocarditis
|
|
NetPath Pathway
|
IL2 Signaling PathwayNetPath_11:TCR Signaling Pathway
|
|
IL2 Signaling PathwayNetPath_23:TSH Signaling Pathway
|
|
IL2 Signaling Pathway
|
|
TGF_beta_Receptor Signaling Pathway
|
|
PANTHER Pathway
|
Angiogenesis
|
|
Cadherin signaling pathway
|
|
Integrin signalling pathway
|
|
Parkinson disease
|
|
CCKR signaling map STP00008:Axon guidance mediated by Slit/RoboP00049:Parkinson disease
|
|
T cell activationP00007:Axon guidance mediated by semaphorins
|
|
Pathway Interaction Database
|
Endothelins
|
|
Signaling events mediated by PRL
|
|
LPA receptor mediated events
|
|
Atypical NF-kappaB pathway
|
|
Glypican 1 network
|
|
Plasma membrane estrogen receptor signaling
|
|
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
|
|
Signaling events mediated by PTP1B
|
|
S1P3 pathway
|
|
EPHB forward signaling
|
|
Nectin adhesion pathway
|
|
Regulation of p38-alpha and p38-beta
|
|
CDC42 signaling events
|
|
Signaling events regulated by Ret tyrosine kinase
|
|
Arf6 signaling events
|
|
Signaling events mediated by TCPTP
|
|
FAS (CD95) signaling pathway
|
|
Thromboxane A2 receptor signaling
|
|
Netrin-mediated signaling events
|
|
Alpha9 beta1 integrin signaling events
|
|
CXCR4-mediated signaling events
|
|
EGF receptor (ErbB1) signaling pathway
|
|
Class I PI3K signaling events
|
|
Posttranslational regulation of adherens junction stability and dissassembly
|
|
Regulation of Androgen receptor activity
|
|
E-cadherin signaling in the nascent adherens junction
|
|
amb2 Integrin signaling
|
|
Integrins in angiogenesis
|
|
ErbB1 downstream signaling
|
|
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
|
|
ErbB2/ErbB3 signaling events
|
|
EPHA forward signaling
|
|
E-cadherin signaling in keratinocytes
|
|
PDGFR-beta signaling pathway
|
|
Nongenotropic Androgen signaling
|
|
Internalization of ErbB1
|
|
CXCR3-mediated signaling events
|
|
Signaling events mediated by VEGFR1 and VEGFR2
|
|
Syndecan-2-mediated signaling events
|
|
Class I PI3K signaling events mediated by Akt
|
|
Syndecan-3-mediated signaling events
|
|
Ephrin B reverse signaling
|
|
Trk receptor signaling mediated by PI3K and PLC-gamma
|
|
EPHA2 forward signaling
|
|
Alpha-synuclein signaling
|
|
FGF signaling pathway
|
|
Alpha4 beta1 integrin signaling events
|
|
Signaling events mediated by focal adhesion kinasep73pathway:p73 transcription factor network
|
|
ATM pathway
|
|
Regulation of Telomerase
|
|
Lissencephaly gene (LIS1) in neuronal migration and development
|
|
Neurotrophic factor-mediated Trk receptor signaling
|
|
Validated transcriptional targets of TAp63 isoforms
|
|
p53 pathway
|
|
Regulation of retinoblastoma proteinnfkappabatypicalpathway:Atypical NF-kappaB pathway
|
|
TCR signaling in naï
|
|
IL12-mediated signaling events
|
|
TCR signaling in naï
|
|
SHP2 signaling
|
|
IL2-mediated signaling events
|
|
IL2 signaling events mediated by PI3K
|
|
IL2 signaling events mediated by STAT5
|
|
Alpha-synuclein signalingfcer1pathway:Fc-epsilon receptor I signaling in mast cells
|
|
ErbB4 signaling events
|
|
Ephrin A reverse signaling
|
|
Reelin signaling pathway
|
|
Angiopoietin receptor Tie2-mediated signaling
|
|
Nephrin/Neph1 signaling in the kidney podocyte
|
|
Signaling events mediated by focal adhesion kinase
|
|
PathWhiz Pathway
|
Fc Epsilon Receptor I Signaling in Mast Cells
|
|
Reactome
|
Regulation of actin dynamics for phagocytic cup formation
|
|
CDO in myogenesis
|
|
RHO GTPases Activate WASPs and WAVEs
|
|
HDR through Single Strand Annealing (SSA)
|
|
Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks
|
|
Factors involved in megakaryocyte development and platelet productionR-HSA-114604:GPVI-mediated activation cascade
|
|
PIP3 activates AKT signaling
|
|
Regulation of KIT signaling
|
|
Phosphorylation of CD3 and TCR zeta chains
|
|
Translocation of ZAP-70 to Immunological synapse
|
|
Generation of second messenger molecules
|
|
PECAM1 interactions
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
DAP12 signaling
|
|
CD28 co-stimulation
|
|
CD28 dependent PI3K/Akt signaling
|
|
CD28 dependent Vav1 pathway
|
|
CTLA4 inhibitory signaling
|
|
PD-1 signaling
|
|
Interleukin-2 signalingR-HSA-114604:GPVI-mediated activation cascade
|
|
Cell surface interactions at the vascular wall
|
|
FCGR activation
|
|
EPH-Ephrin signaling
|
|
Role of LAT2/NTAL/LAB on calcium mobilization
|
|
Nephrin interactions
|
|
NCAM signaling for neurite out-growth
|
|
EPHB-mediated forward signaling
|
|
EPHA-mediated growth cone collapse
|
|
EPH-ephrin mediated repulsion of cells
|
|
CRMPs in Sema3A signaling
|
|
DCC mediated attractive signaling
|
|
Netrin mediated repulsion signals
|
|
VEGFA-VEGFR2 Pathway
|
|
Dectin-2 family
|
|
CD209 (DC-SIGN) signaling
|
|
RAF/MAP kinase cascade
|
|
Platelet Adhesion to exposed collagen
|
|
Regulation of signaling by CBL
|
|
Antigen activates B Cell Receptor (BCR) leading to generation of second messengers
|
|
WikiPathways
|
ErbB Signaling Pathway
|
|
Senescence and Autophagy in Cancer
|
|
Notch Signaling Pathway
|
|
EPO Receptor Signaling
|
|
EGF/EGFR Signaling Pathway
|
|
TGF beta Signaling Pathway
|
|
Signaling of Hepatocyte Growth Factor Receptor
|
|
Kit receptor signaling pathway
|
|
Pregnane X Receptor pathway
|
|
Aryl Hydrocarbon Receptor Pathway
|
|
IL-3 Signaling Pathway
|
|
Nanoparticle-mediated activation of receptor signaling
|
|
Polycystic Kidney Disease Pathway
|
|
Alpha 6 Beta 4 signaling pathway
|
|
BDNF signaling pathway
|
|
Integrated Pancreatic Cancer Pathway
|
|
Oncostatin M Signaling Pathway
|
|
Interleukin-11 Signaling Pathway
|
|
AGE/RAGE pathway
|
|
Signaling Pathways in Glioblastoma
|
|
TSLP Signaling Pathway
|
|
Arylhydrocarbon receptor (AhR) signaling pathway
|
|
Regulation of Microtubule Cytoskeleton
|
|
FSH signaling pathway
|
|
Leptin signaling pathway
|
|
RANKL/RANK Signaling Pathway
|
|
Integrin-mediated Cell Adhesion
|
|
Angiogenesis
|
|
Androgen receptor signaling pathwayWP2864:Apoptosis-related network due to altered Notch3 in ovarian cancer
|
|
Fcgamma receptor (FCGR) dependent phagocytosis
|
|
ATM Signaling Pathway
|
|
Retinoblastoma (RB) in Cancer
|
|
Pathogenic Escherichia coli infection
|
|
Integrated Breast Cancer Pathway
|
|
Signaling by Robo receptor
|
|
Myogenesis
|
|
Factors involved in megakaryocyte development and platelet productionWP61:Notch Signaling Pathway
|
|
Interferon type I signaling pathways
|
|
IL-2 Signaling Pathway
|
|
Inflammatory Response Pathway
|
|
Signaling by SCF-KIT
|
|
DAP12 interactions
|
|
Host Interactions of HIV factors
|
|
PIP3 activates AKT signaling
|
|
T-Cell Receptor and Co-stimulatory Signaling
|
|
B Cell Receptor Signaling Pathway
|
|
TCR signaling
|
|
Costimulation by the CD28 familyWP69:TCR Signaling Pathway
|
|
Ectoderm Differentiation
|
|
Fc epsilon receptor (FCERI) signaling
|
|
Signaling by the B Cell Receptor (BCR)
|
|
Primary Focal Segmental Glomerulosclerosis FSGS
|
|
IL-7 Signaling Pathway
|
|
Semaphorin interactions
|
|
Platelet Adhesion to exposed collagen
|
|
Netrin-1 signaling
|
|
Nephrin interactions
|
|
NCAM signaling for neurite out-growth
|
|
GPVI-mediated activation cascade
|
|
Costimulation by the CD28 family
|
|
Cell surface interactions at the vascular wall
|
| References |
| REF 1 | 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101. |
|---|
| REF 2 | Dasatinib: a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome-positive acute lymphoblastic leukemia. Clin Ther. 2007 Nov;29(11):2289-308. |
|---|
| REF 3 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5678). |
|---|
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 |
|---|
| REF 5 | Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27. |
|---|
| REF 6 | Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. |
|---|
| REF 7 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. |
|---|
| REF 8 | In vitro and clinical investigation of the relationship between CCR5 receptor occupancy and anti-HIV activity of Aplaviroc. J Clin Pharmacol. 2008 Oct;48(10):1179-88. Epub 2008 Aug 1. |
|---|
