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AZD7545

Catalog No. T2447   CAS 252017-04-2

AZD7545 is a potent PDHK inhibitor.

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AZD7545 Chemical Structure
AZD7545, CAS 252017-04-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
2 mg In stock $ 57.00
5 mg In stock $ 94.00
10 mg In stock $ 158.00
25 mg In stock $ 279.00
50 mg In stock $ 415.00
100 mg In stock $ 589.00
1 mL * 10 mM (in DMSO) In stock $ 113.00
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Purity: 98.69%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AZD7545 is a potent PDHK inhibitor.
Targets&IC50 PDHK2:6.4 nM, PDHK1:36.8 nM
Kinase Assay Cellular Kinase Assays: NIH3T3 cells prepared by transfection of human KDR. The cells are cultured in a collagen type I coated 96-well plate in an amount of 1.5 × 104 per well. The medium is then replaced by a DMEM medium containing 0.1% FCS. Ki8751 diluted in DMSO is added to each well and cultured. rhVEGF is added to a final concentration of 100 ng/mL, and the stimulation of cells is carried out at 37 °C. The cells are washed with PBS (pH 7.4), 50 μL of a solubilization buffer (20 mM HEPES (pH 7.4), 150 mM NaCl, 0.2% Triton X-100, 10% glycerol, 5 mM Na3VO4, 5 mM disodium ethylenediamine tetraacetate, and 2 mM Na4P2O7) is then added and a cell extract is prepared. Separately, PBS (50 μL, pH 7.4) containing 5 μg/mL of antiphosphotyrosine antibody (PY20) is added to a microplate for ELISA. After washing of the plate, 300 μL of a blocking solution is added. The cell extract is transferred to the plate. An anti-VEGFR2 antibody and a peroxidase-labeled anti-rabbit Ig antibody are added. Next, a chromophoric substrate for peroxidase is added, and the absorbance at 450 nm is measured with microplate reader. The VEGFR2 phosphorylation activity for each well is determined by presuming the absorbance with the addition of VEGF and without the addition of the test sample to be 100% VEGFR2 phosphorylation activity and VEGF to be 0% VEGFR2 phosphorylation activity. The concentration of the inhibition (%) of VEGFR2 Phosphorylation is determined for each case, and IC50 value is calculated.
Molecular Weight 478.87
Formula C19H18ClF3N2O5S
CAS No. 252017-04-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 88 mg/mL (183.8 mM)

DMSO: 88 mg/mL (183.8 mM)

TargetMolReferences and Literature

1. Morrell JA, et al. Biochem Soc Trans. 2003, 31(Pt 6), 1168-1170. 2. Mayers RM, et al. Biochem Soc Trans. 2003, 31(Pt 6), 1165-1167. 3. Tuganova A, et al. Biochemistry. 2007, 46(29), 8592-8602.

Related compound libraries

This product is contained In the following compound libraries:
ReFRAME Related Library Bioactive Compounds Library Max Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Fluorochemical Library Target-Focused Phenotypic Screening Library Glycolysis Compound Library Mitochondria-Targeted Compound Library Metabolism Compound Library Kinase Inhibitor Library

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Keywords

AZD7545 252017-04-2 Metabolism Dehydrogenase PDH kinase AZD 7545 AZD-7545 inhibit PDHK Pyruvate dehydrogenase kinase Inhibitor inhibitor

 

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