Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T649279-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $130.90 | |
T649279-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $210.90 | |
T649279-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $740.90 | |
T649279-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,200.90 |
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 |
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Specifications & Purity | ≥99% |
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 |
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 ) |
ALogP | 2.4 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-[5-[2-(cyclopropanecarbonylamino)imidazo[1,2-b]pyridazin-6-yl]oxy-2-methylphenyl]-2,5-dimethylpyrazole-3-carboxamide |
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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) |
InChi Key | DZFZXPPHBWCXPQ-UHFFFAOYSA-N |
Canonical 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 |
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Solubility | DMSO : ≥ 48.5 mg/mL (108.87 mM) |
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