iMDK 是一种有效的PI3K抑制剂，可抑制生长因子MDK（也称为中期因子或 MK）。iMDK 与 MEK 抑制剂协同抑制非小细胞肺癌 (NSCLC)，而不会伤害正常细胞和小鼠。
| 生物活性 | iMDK is a potentPI3Kinhibitor and inhibits the growth factorMDK(also known asmidkineor MK). iMDK suppresses non-small cell lungcancer(NSCLC) cooperatively with AMEK inhibitorwithout harming normal cells and mice[1]. |
体外研究
(In Vitro) | iMDK (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[1].
Cell Viability Assay[1] | Cell Line: | H441 (lung adenocarcinoma; KRASG12V), H2009 (non-small cell carcinoma; KRASG12A), A549 (lung carcinoma; KRASG12S) and H520 (lung squamous cell carcinoma; KRASWT) | | 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 Analysis[1] | Cell 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. |
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体内研究
(In Vivo) | The 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[1].
| Animal Model: | female BALB/c nude mice (6 week old) bearing H441 human lung cancer xenografts[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 3.33 mg/mL(8.85 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.6567 mL | 13.2837 mL | 26.5675 mL | | 5 mM | 0.5313 mL | 2.6567 mL | 5.3135 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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