| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| 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].
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|---|---|
| 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]. Naomasa Ishida, et al. 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.
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| Molecular Formula |
C21H13FN2O2S.1/4H20
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|---|---|
| Molecular Weight |
380.91
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| Related CAS # |
iMDK;881970-80-5
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| 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)
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| Solubility (In Vitro) |
DMSO :~3.33 mg/mL (~8.74 mM)
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|---|---|
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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