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TAK-593 - 99%, high purity , Vascular endothelial growth factor receptor inhibitor, CAS No.1005780-62-0, Vascular endothelial growth factor receptor inhibitor

COA COA
In stock
Item Number
T649279
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T649279-1mg
1mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$19.90
T649279-5mg
5mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$58.90
T649279-25mg
25mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$199.90
T649279-100mg
100mg
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$454.90
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View related series
PDGFR (109) Protein Tyrosine Kinase/RTK (1314) Receptor Tyrosine Kinase (1260) VEGFR (187)

Basic Description

Synonyms C13977 | N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide | NSC800939 | NSC-800939 | DB13093 | DZFZXPPHBWCXPQ-UHFFFAOYSA-N | MS-28025 | TAK-593 | NCGC00485933-01 | UNII-H3I42X8XX
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC 50 s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1 , VEGFR2 , VEGFR3 , PDFGRα and PDFGRβ, respectively.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Vascular endothelial growth factor receptor inhibitor
Product Description

TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC 50 s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.

In Vitro

TAK-593 inhibits growth of HUVEC with an IC 50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC 50 =3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC 50 =4.3, 13 nM) families. Against other kinases, the IC 50 values of TAK-593 are above 100 nM, except for Fms (IC 50 =10 nM) and Ret (IC 50 =18 nM) kinases. TAK-593 potently inhibits VEGF- and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TAK-593 inhibits growth of HUVEC with an IC 50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC 50 =3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC 50 =4.3, 13 nM) families. Against other kinases, the IC 50 values of TAK-593 are above 100 nM, except for Fms (IC 50 =10 nM) and Ret (IC 50 =18 nM) kinases . TAK-593 potently inhibits VEGF- and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:VEGFR1 3.2 nM (IC 50 ) VEGFR2 0.95 nM (IC 50 ) VEGFR3 1.1 nM (IC 50 ) PDGFRα 4.3 nM (IC 50 ) PDGFRβ 13 nM (IC 50 ) PDGFRα V561D 1 nM (IC 50 )

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Anilides
Intermediate Tree Nodes Not available
Direct Parent Aromatic anilides
Alternative Parents Diarylethers  2-heteroaryl carboxamides  N-arylamides  Phenol ethers  Phenoxy compounds  Pyrazole-5-carboxamides  Toluenes  N-substituted imidazoles  Imidolactams  Cyclopropanecarboxylic acids and derivatives  Pyridazines and derivatives  Heteroaromatic compounds  Secondary carboxylic acid amides  Azacyclic compounds  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Aromatic anilide - Diaryl ether - 2-heteroaryl carboxamide - Phenol ether - Phenoxy compound - Pyrazole-5-carboxamide - N-arylamide - Toluene - Pyridazine - Cyclopropanecarboxylic acid or derivatives - N-substituted imidazole - Imidolactam - Azole - Pyrazole - Imidazole - Heteroaromatic compound - Carboxamide group - Secondary carboxylic acid amide - Carboxylic acid derivative - Ether - Azacycle - Organoheterocyclic compound - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Carbonyl group - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group.
External Descriptors Not available

Product Properties

ALogP 2.4

Associated Targets(Human)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT4 Tclin Vascular endothelial growth factor receptor 3 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDGFRA Tclin Platelet-derived growth factor receptor alpha (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDGFRB Tclin Platelet-derived growth factor receptor beta (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
BCR Tclin Breakpoint cluster region protein (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
Tchem Uncharacterized protein FLJ45252 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TOP2A Tclin DNA topoisomerase II alpha (6317 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IMPDH2 Tclin Inosine-5'-monophosphate dehydrogenase 2 (1326 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DCK Tchem Deoxycytidine kinase (530 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NQO2 Tchem Quinone reductase 2 (885 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AK2 Tbio Adenylate kinase 2 (264 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKACB Tchem cAMP-dependent protein kinase beta-1 catalytic subunit (589 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKAG1 Tchem AMP-activated protein kinase, gamma-1 subunit (254 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K3 Tchem Dual specificity mitogen-activated protein kinase kinase 3 (632 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK6 Tclin Cyclin-dependent kinase 6 (1724 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKAG2 Tchem AMP-activated protein kinase, gamma-2 subunit (243 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GRK2 Tchem G-protein coupled receptor kinase 2 (1019 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PYGB Tchem Brain glycogen phosphorylase (474 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKD3 Tchem Protein kinase C nu (2315 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PFKP Tbio Phosphofructokinase platelet type (224 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1E Tclin Casein kinase I epsilon (1412 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK4 Tbio CaM kinase IV (2116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT1 Tclin Vascular endothelial growth factor receptor 1 (6262 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3A Tclin Glycogen synthase kinase-3 alpha (3764 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Cdk4 Cyclin-dependent kinase 4 (3 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Pygl Liver glycogen phosphorylase (81 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cynomolgus monkey (4946 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AIRC Multifunctional protein ADE2 (8 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Lung (9 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Septin9 Septin-9 (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Acadvl Very long-chain specific acyl-CoA dehydrogenase, mitochondrial (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 24767976
IUPAC Name N-[5-[2-(cyclopropanecarbonylamino)imidazo[1,2-b]pyridazin-6-yl]oxy-2-methylphenyl]-2,5-dimethylpyrazole-3-carboxamide
INCHI InChI=1S/C23H23N7O3/c1-13-4-7-16(11-17(13)24-23(32)18-10-14(2)27-29(18)3)33-21-9-8-20-25-19(12-30(20)28-21)26-22(31)15-5-6-15/h4,7-12,15H,5-6H2,1-3H3,(H,24,32)(H,26,31)
InChIKey DZFZXPPHBWCXPQ-UHFFFAOYSA-N
Smiles CC1=C(C=C(C=C1)OC2=NN3C=C(N=C3C=C2)NC(=O)C4CC4)NC(=O)C5=CC(=NN5C)C
Isomeric SMILES CC1=C(C=C(C=C1)OC2=NN3C=C(N=C3C=C2)NC(=O)C4CC4)NC(=O)C5=CC(=NN5C)C
Alternate CAS 1005780-62-0
PubChem CID 24767976
MeSH Entry Terms TAK 593;TAK-593;TAK593
Molecular Weight 445.47

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : ≥ 48.5 mg/mL (108.87 mM)
Molecular Weight 445.500 g/mol
XLogP3 2.400
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 6
Exact Mass 445.186 Da
Monoisotopic Mass 445.186 Da
Topological Polar Surface Area 115.000 Ų
Heavy Atom Count 33
Formal Charge 0
Complexity 735.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
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