1. PI3K/Akt/mTOR
  2. PI3K
  3. iMDK

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.

For research use only. We do not sell to patients.

iMDK Chemical Structure

iMDK Chemical Structure

CAS No. : 881970-80-5

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

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].

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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (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[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.
Molecular Weight

376.40

Formula

C21H13FN2O2S

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1C(C2=CN3C(SC(CC4=CC=C(F)C=C4)=C3)=N2)=CC5=CC=CC=C5O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (5.31 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6567 mL 13.2837 mL 26.5675 mL
5 mM 0.5313 mL 2.6567 mL 5.3135 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6567 mL 13.2837 mL 26.5675 mL 66.4187 mL
5 mM 0.5313 mL 2.6567 mL 5.3135 mL 13.2837 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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iMDK
Cat. No.:
HY-110171
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