705946-27-6
705946-27-6 structure
- Name: Tyrosine kinase-IN-1
- Chemical Name: Tyrosine kinase-IN-1
- CAS Number: 705946-27-6
- Molecular Formula: C26H28FN5O
- Molecular Weight: 445.532
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-02-17 23:42:32
- Modify Date: 2024-01-08 16:09:41
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Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
| Name | Tyrosine kinase-IN-1 |
|---|---|
| Synonyms |
(3Z)-5-[(1-Ethyl-4-piperidinyl)amino]-3-[(3-fluorophenyl)(5-methyl-1H-imidazol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one
2H-Indol-2-one, 5-[(1-ethyl-4-piperidinyl)amino]-3-[(3-fluorophenyl)(5-methyl-1H-imidazol-2-yl)methylene]-1,3-dihydro-, (3Z)- (3Z)-5-[(1-Ethyl-4-piperidinyl)amino]-3-[(3-fluorophenyl)(4-methyl-1H-imidazol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one 6I7PLF6N8L |
| Description | Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively. |
|---|---|
| Related Catalog | |
| Target |
Flt-1:4 nM (IC50) KDR:20 nM (IC50) PDGFRα:4 nM (IC50) FGFR1:2 nM (IC50) |
| In Vitro | Tyrosine kinase-IN-1 is from reference (compound 8K)[1]. |
| In Vivo | Tyrosine kinase-IN-1 shows a reasonable PK profile (AUC(0–∞)=1.9, t1/2=4.6 h). It has a favorable oral bioavailability (F=63%) in rats[1]. |
| Kinase Assay | Kinase Inhibition Assays Kinase activities of KDR and PDGFRα are measured as the percent of ATP consumed following the kinase reaction using luciferaseluciferin-coupled chemiluminescence. Kinase reactions are initiated by combining test compound (Tyrosine kinase-IN-1), ATP, kinases and substrates in a 20 mL volume using 384-well microtiter plates. For KDR, the final reaction mixture contained 3 mM ATP, 1.6 mM poly(Glu, Tyr) 4:1 and 1.5 nM KDR of residues D807-V1356 with an N-terminal GST tag. For PDGFRα, the final reaction mixture contained 2 mM ATP, 10 mM MBP and 14 nM PDGFRα of residues Q551-L1089 with an N-terminal GST tag. The reaction mixture is incubated at room temperature for 4 h (KDR) or 2 h PDGFRα before a 20 mL aliquot of Kinase Glo is added and luminescence signal is measured using a Victor2 plate reader. Total ATP consumption is limited below 50%[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C26H28FN5O |
| Molecular Weight | 445.532 |
| Exact Mass | 445.227783 |
| LogP | 2.59 |
| Index of Refraction | 1.652 |
| Storage condition | 2-8℃ |