iMDK

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

iMDK 

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。

iMDK

iMDK Chemical Structure

CAS No. : 881970-80-5

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iMDK 的其他形式现货产品:

iMDK quarterhydrate

生物活性

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[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].

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) 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.

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) 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.

分子量

376.40

Formula

C21H13FN2O2S
CAS 号

881970-80-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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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