iMDK quarterhydrate is a potent PI3K inhibitor that suppresses the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate synergistically inhibits non-small cell lung cancer (NSCLC) with MEK inhibitors without harming normal cells and mice.

Physicochemical Properties

Molecular Formula	C21H13FN2O2S.1/4H20
Molecular Weight	380.91
Related CAS #	iMDK;881970-80-5
Appearance	White to light yellow solid powder
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	After 72 hours of treatment, iMDK (50-500 nM) tetrahydrate reduced AKT phosphorylation in H441 lung adenocarcinoma cells in a dose-dependent manner. On the other hand, p-ERK is greatly increased by iMDK quarterhydrate[1].
ln Vivo	In a xenograft mouse model, combined therapy with iMDK (9 mg/kg/day; 100 ul i.p.) and PD0325901 (5 mg/kg; oral) substantially inhibited the formation of lung tumors [1].
Cell Assay	Cell Viability Assay[1] Cell Types: H441(lung adenocarcinoma; KRASG12V), H2009(non-small cell carcinoma; KRASG12A), A549(lung carcinoma; KRASG12S) and H520(lung squamous cell carcinoma; KRASWT) Tested Concentrations: iMDK(2.5 μM) quarterhydrate and PD0325901(0.5 μM) for H441 and H2009 cells iMDK(0.125 μM) quarterhydrate and PD0325901(0.25 μM) for H520 cells iMDK(0.25 μM) quarterhydrate and PD0325901(0.125 μM) for A549 cells Incubation Duration: 72 hrs (hours) Experimental Results: iMDK quarterhydrate alone did not inhibit cell viability of A549 cells, the combinatorial treatment of iMDK quarterhydrate with PD0325901 Dramatically inhibited that of A549 cells compared to the single treatment of PD0325901. Western Blot Analysis[1] Cell Types: H441 lung adenocarcinoma cells Tested Concentrations: 0-500 nM Incubation Duration: 72 hrs (hours) Experimental Results: Suppressed AKT phosphorylation in a dose-dependent manner. ERK1/2 phosphorylation was increased.
Animal Protocol	Animal/Disease Models: female BALB/c nude mice (6 week old) bearing H441 human lung cancer xenografts[1] Doses: iMDK (9 mg/kg) quarterhydrate and PD0325901 (5 mg/kg) Route of Administration: intraperitoneally (ip) injected with 100 μL iMDK everyday and/or orally Experimental Results: decreased Dramatically volume of the tumors derived from H441 lung adenocarcinoma cells after the combination treatment with iMDK quarterhydrate and PD0325901 compared to that of single compound in a xenograft mouse model.
References	[1]. A novel PI3K inhibitor iMDK suppresses non-small cell lung Cancer cooperatively with A MEK inhibitor. Exp Cell Res. 2015 Jul 15;335(2):197-206.

Solubility Data

Solubility (In Vitro)	DMSO :~3.33 mg/mL (~8.74 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 2 mg/mL (5.25 mM) in Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6253 mL	13.1265 mL	26.2529 mL
	5 mM	0.5251 mL	2.6253 mL	5.2506 mL
	10 mM	0.2625 mL	1.3126 mL	2.6253 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.