iMDK (C09-1140-034)

iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice.In VitroiMDK (50–500 nM) suppressed AKT phosphorylation in a dose-dependent manner in H441 lung adenocarcinoma cells after treatment for 72 h. In contrast, iMDK robustly increases p-ERK. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: H441 (lung adenocarcinoma; KRAS G12V ), H2009 (non-small cell carcinoma; KRAS G12A ), A549 (lung carcinoma; KRAS G12S ) and H520 (lung squamous cell carcinoma; KRAS WT ) Concentration: iMDK (2.5 μM) and PD0325901 (0.5 μM) for H441 and H2009 cells iMDK (0.125 μM) and PD0325901 (0.25 μM) for H520 cells iMDK (0.25 μM) and PD0325901 (0.125 μM) for A549 cells Incubation Time: 72 hours Result: iMDK alone did not inhibit cell viability of A549 cells, the combinatorial treatment of iMDK with PD0325901 significantly inhibited that of A549 cells compared to the single treatment of PD0325901. Western Blot AnalysisCell Line: H441 lung adenocarcinoma cells Concentration: 0-500 nM Incubation Time: 72 hours Result: Suppressed AKT phosphorylation in a dose-dependent manner. ERK1/2 phosphorylation was increased.In VivoThe combination treatment of iMDK ( (9 mg/kg/day; intraperitoneally injected with 100 μl) and PD0325901 (5 mg/kg; orally administered) effectively reduced lung tumor growth in a xenograft mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: female BALB/c nude mice (6 week old) bearing H441 human lung cancer xenografts Dosage: iMDK (9 mg/kg) and PD0325901 (5 mg/kg) Administration: Intraperitoneally injected with 100 μL iMDK everyday and/or orally administered PD0325901 five times per week (on days 1, 2, 3, 4, 5, 7, 8, 9, 10, 11) Result: Reduced significantly volume of the tumors derived from H441 lung adenocarcinoma cells after the combination treatment with iMDK and PD0325901 compared to that of single compound in a xenograft mouse model.Form:Solid. Specifications and Purity: 99%. Molecular Formula: C21H13FN2O2S. Molecular Weight: 376.4. PubChem CID: 15991416. Isomeric SMILES: C1=CC=C2C(=C1)C=C(C(=O)O2)C3=CN4C=C(SC4=N3)CC5=CC=C(C=C5)F.