BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases the inhibitory activity of human Ether-a-go-go-related gene (hERG) with IC50 of 1.52 μM. BKI-13699 reduces parasite burden and disease severity in a reproductive pig model. BKI-1369 has been fully characterized for potency, stability, metabolism, toxicity and pharmacokinetics and is effective against Cryptosporidium parvum (C. parvum) in infected mice and calves.

Physicochemical Properties

Molecular Formula	C23H27N7O
Molecular Weight	417.506783723831
Exact Mass	417.227
CAS #	1951431-22-3
PubChem CID	122453014
Appearance	White to off-white solid powder
LogP	3.2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	5
Heavy Atom Count	31
Complexity	586
Defined Atom Stereocenter Count	0
InChi Key	AWJAAKKEYXUCFY-UHFFFAOYSA-N
InChi Code	InChI=1S/C23H27N7O/c1-3-31-19-7-5-16-12-17(4-6-18(16)27-19)21-20-22(24)25-14-26-23(20)30(28-21)13-15-8-10-29(2)11-9-15/h4-7,12,14-15H,3,8-11,13H2,1-2H3,(H2,24,25,26)
Chemical Name	3-(2-ethoxyquinolin-6-yl)-1-[(1-methylpiperidin-4-yl)methyl]pyrazolo[3,4-d]pyrimidin-4-amine
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

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~119.76 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 5 mg/mL (11.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 50.0 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. Solubility in Formulation 2: ≥ 5 mg/mL (11.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3952 mL	11.9758 mL	23.9515 mL
	5 mM	0.4790 mL	2.3952 mL	4.7903 mL
	10 mM	0.2395 mL	1.1976 mL	2.3952 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.