iMDK quarterhydrate

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iMDK quarterhydrate  纯度: ≥99.0%

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。

iMDK quarterhydrate

iMDK quarterhydrate Chemical Structure

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
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50 mg   询价  

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iMDK quarterhydrate 相关产品

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生物活性

iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 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[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.

分子量

380.91

Formula

C21H15FN2O3S
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
溶解性数据
In Vitro: 

DMSO : 12.8 mg/mL (33.60 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 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

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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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