VER 246608

Name: VER 246608
Brand: Tocris Bioscience
SKU: 6604

Tocris Bioscience, part of Bio-Techne | Catalog # 6604

COA / SDS

Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor

Key Product Details

Description:	Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor
Chemical Name:	N-[4-(2-Chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
Purity:	≥98% (HPLC)
Molecular Weight:	552.96

View Full Technical Details for VER 246608

Technical Data
Citations

Biological Activity for VER 246608

VER 246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK; IC₅₀s = 35, 40, 84, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4 respectively). It is selective for PDKs over a panel of 97 kinases and HSP90. VER 246608 increases pyruvate dehydrogenase complex activity, oxygen consumption and reduces glycolytic activity; it reduces the production of L-lactate in PC3 cells in D-glucose and L-glutamine depleted media. In PC3 cells, VER 246608 induces cell cycle arrest at the G₁ phase under glucose or serum-depleted conditions characteristic of the tumor microenvironment.

Compound Libraries for VER 246608

VER 246608 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for VER 246608

M. Wt	552.96
Formula	C₂₈H₂₃ClF₂N₄O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1684386-71-7
PubChem ID	86280454
InChi Key	LCGNLQSOSJFLKR-UHFFFAOYSA-N
Smiles	O=C(C1=CC=C(O)C=C1O)N(C=2C=CC(=CC2)C3=NC(Cl)=NC=C3C)CC4=CC=C(C=C4)CNC(=O)C(F)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for VER 246608

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	55.3	100

Preparing Stock Solutions for VER 246608

The following data is based on the product molecular weight 552.96.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.81 mL	9.04 mL	18.08 mL
5 mM	0.36 mL	1.81 mL	3.62 mL
10 mM	0.18 mL	0.90 mL	1.81 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for VER 246608

References are publications that support the biological activity of the product.

Moore VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget 2014 PMID: 25404640
Brough Application of off-rate screening in the identification of novel pan- isoform inhibitors of pyruvate dehydrogenase kinase. J.Med.Chem. 2017 PMID: 28199108