ChemicalBook > CAS DataBase List > TAK-593

TAK-593

Product Name
TAK-593
CAS No.
1005780-62-0
Chemical Name
TAK-593
Synonyms
TAK-593;TAK-593, 10 mM in DMSO;N-(5-((2-(Cyclopropanecarboxamido)imidazo[1,2-b]pyridazin-6-yl)oxy)-2-methylphenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide;1H-Pyrazole-5-carboxamide, N-[5-[[2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl]oxy]-2-methylphenyl]-1,3-dimethyl-;Platelet-derived growth factor receptor,VEGFR,PDGFR,Inhibitor,TAK 593,inhibit,TAK593,TAK-593,Vascular endothelial growth factor receptor
CBNumber
CB52667086
Molecular Formula
C23H23N7O3
Formula Weight
445.47
MOL File
1005780-62-0.mol
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TAK-593 Property

Density 
1.46±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Solid
pka
9.22±0.20(Predicted)
color 
White to light yellow
InChIKey
DZFZXPPHBWCXPQ-UHFFFAOYSA-N
SMILES
N1(C)C(C(NC2=CC(OC3=NN4C=C(NC(C5CC5)=O)N=C4C=C3)=CC=C2C)=O)=CC(C)=N1
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-2403
Product name
TAK-593
Purity
99.62%
Packaging
5mg
Price
$180
Updated
2021/12/16
ChemScene
Product number
CS-2403
Product name
TAK-593
Purity
99.62%
Packaging
10mg
Price
$300
Updated
2021/12/16
ChemScene
Product number
CS-2403
Product name
TAK-593
Purity
99.62%
Packaging
50mg
Price
$936
Updated
2021/12/16
ChemScene
Product number
CS-2403
Product name
TAK-593
Purity
99.62%
Packaging
100mg
Price
$1440
Updated
2021/12/16
Crysdot
Product number
CD31004878
Product name
TAK-593
Purity
98+%
Packaging
50mg
Price
$840
Updated
2021/12/16
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TAK-593 Chemical Properties,Usage,Production

Uses

TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.

in vivo

TAK-593 inhibits growth of HUVEC with an IC50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC50=3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC50=4.3, 13 nM) families. Against other kinases, the IC50 values of TAK-593 are above 100 nM, except for Fms (IC50=10 nM) and Ret (IC50=18 nM) kinases[1]. 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[2].

IC 50

VEGFR1: 3.2 nM (IC50); VEGFR2: 0.95 nM (IC50); VEGFR3: 1.1 nM (IC50); PDGFRα: 4.3 nM (IC50); PDGFRβ: 13 nM (IC50); PDGFRαV561D: 1 nM (IC50)

References

[1] Miyamoto N, et al. Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor. Bioorg Med Chem. 2013 Apr 15;21(8):2333-2345. DOI:10.1016/j.bmc.2013.01.074
[2] Awazu Y, et al. Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013 Apr;104(4):486-94. DOI:10.1111/cas.12101

TAK-593 Preparation Products And Raw materials

Raw materials

Preparation Products

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TAK-593 Suppliers

CHINA 43 United States 4 Global 47
MQ (shanghai) Pharmaceuticals Co., Ltd.
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InvivoChem
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1005780-62-0, TAK-593Related Search:


  • TAK-593
  • 1H-Pyrazole-5-carboxamide, N-[5-[[2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl]oxy]-2-methylphenyl]-1,3-dimethyl-
  • Platelet-derived growth factor receptor,VEGFR,PDGFR,Inhibitor,TAK 593,inhibit,TAK593,TAK-593,Vascular endothelial growth factor receptor
  • N-(5-((2-(Cyclopropanecarboxamido)imidazo[1,2-b]pyridazin-6-yl)oxy)-2-methylphenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide
  • TAK-593, 10 mM in DMSO
  • 1005780-62-0