VI 16832 is a broad spectrum (a wide range) type I kinase inhibitor that can be used as an enrichment tool for comparative expression analysis of protein kinases in different cancer/tumor cell lines.

Physicochemical Properties

Molecular Formula	C22H25N5O2
Molecular Weight	391.466204404831
Exact Mass	391.2
CAS #	1430218-51-1
PubChem CID	89510076
Appearance	Light yellow to yellow solid powder
Density	1.3±0.1 g/cm3
Boiling Point	611.9±65.0 °C at 760 mmHg
Flash Point	323.9±34.3 °C
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.679
LogP	1.87
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	6
Heavy Atom Count	29
Complexity	620
Defined Atom Stereocenter Count	0
InChi Key	RCSLGYIVHUXZCI-UHFFFAOYSA-N
InChi Code	InChI=1S/C22H25N5O2/c23-9-10-29-18-6-4-17(5-7-18)25-22-24-13-16-3-8-20(28)27(21(16)26-22)19-12-14-1-2-15(19)11-14/h3-8,13-15,19H,1-2,9-12,23H2,(H,24,25,26)
Chemical Name	2-[4-(2-Aminoethoxy)anilino]-8-(3-bicyclo[2.2.1]heptanyl)pyrido[2,3-d]pyrimidin-7-one
Synonyms	VI16832 VI 16832 VI-16832
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro

VI 16832 is a type I kinase inhibitor with a broad spectrum [1]. More than 8500 phosphopeptides were found by phosphoproteomic analysis of VI 16832-enriched fractions in MV4-11, HCT116, or 435S cells. These correspond to 212 distinct protein kinase superfamily members, or around 1700 distinct phosphopeptide compounds. The overall number of discovered phosphorylation sites on protein kinases was greatly increased by analysis of VI 16832 retained proteins from three cancer cell lines. When calculating the total phosphopeptide intensities to determine the quantity of protein enriched in VI 16832, protein kinases accounted for more than 80% of the total [2].

References

[1]. Proteomic Analysis Defines Kinase Taxonomies Specific for Subtypes of Breast Cancer. Apr. 1, 2017. [2]. Large-scale Proteomics Analysis of the Human Kinome. Mol Cell Proteomics. 2009 Jul; 8(7): 1751-1764.

Solubility Data

Solubility (In Vitro)

DMSO : ~33.33 mg/mL (~85.14 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5545 mL	12.7724 mL	25.5447 mL
	5 mM	0.5109 mL	2.5545 mL	5.1089 mL
	10 mM	0.2554 mL	1.2772 mL	2.5545 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.