iMDK quarterhydrate 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 quarterhydrate 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 quarterhydrate is a potentPI3Kinhibitor and inhibits the growth factorMDK(also known asmidkineor MK). iMDK quarterhydrate 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) quarterhydrate suppressed AKT phosphorylation in a dose-dependent manner in H441 lung adenocarcinoma cells after treatment for 72 h. In contrast, iMDK quarterhydrate 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) 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 Time: | 72 hours | | Result: | iMDK quarterhydrate alone did not inhibit cell viability of A549 cells, the combinatorial treatment of iMDK quarterhydrate 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) quarterhydrate and PD0325901 (5 mg/kg) | | Administration: | Intraperitoneally injected with 100 μL iMDK everyday and/or orally | | Result: | Reduced significantly 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. |
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| Formula | |
| 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 : 20 mg/mL(52.51 mM;Need ultrasonic) 配制储备液 | 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 |
*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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2 mg/mL (5.25 mM); Suspended solution; Need ultrasonic
此方案可获得 2 mg/mL (5.25 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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