Drug Information

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 [528715], [536577], [541021], [551871]
Multiple myeloma [ICD9: 203; ICD10:C90] Phase 2 [536957], [541021]
Therapeutic Class
Anticancer Agents
Company
Bristol Myers Squibb
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
3062316
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 [536331], [536474], [536797]
Proto-oncogene c-Abl Target Info Inhibitor [536331], [536474], [536797]
Lck tyrosine kinase Target Info Inhibitor [536331], [536474], [536797]
Fyn tyrosine kinase Target Info Inhibitor [536331], [536474], [536797]
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 na&#xef
IL12-mediated signaling events
TCR signaling in na&#xef
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 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 536577Dasatinib: 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 536957Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27.
Ref 541021(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 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 536331Multi-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 536474A 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 536797In 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.

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