MP7 (Synonyms: PDK1 inhibitor)

Name: MP7
Brand: MedChemExpress
SKU: HY-14440
Rating: 5.0 (2 reviews)

Cat. No.: HY-14440 Purity: 99.33%: Data Sheet
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MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.

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

MP7 Chemical Structure

CAS No. : 1001409-50-2

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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10 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE MP7

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Biological Activity
Protocol
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Description

MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.

IC₅₀ & Target

PDK1^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human 786-0 cells measured after 72 hrs by MTT assay Cytotoxicity against human 786-0 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
A-427	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human A427 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human A427 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
A549	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human A549 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human A549 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
A673	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human A673 cells measured after 72 hrs by MTT assay Cytotoxicity against human A673 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
BEAS-2B	IC₅₀	96.36 μM Compound: 6; MP7	Antiproliferative against human BEAS-2B cells measured after 48 hrs by CCK8 assay Antiproliferative against human BEAS-2B cells measured after 48 hrs by CCK8 assay	[PMID: 36603508]
BT-474	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human BT474 cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human BT474 cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
CAKI-1	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human CAKI-1 cells measured after 72 hrs by MTT assay Cytotoxicity against human CAKI-1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
HCT-116	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human HCT116 cells harboring PI3KCA/KRAS double mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human HCT116 cells harboring PI3KCA/KRAS double mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
HCT-116	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human HCT-116 cells measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
HFL1	IC₅₀	64.79 μM Compound: 6; MP7	Antiproliferative against HLF1 cells measured after 48 hrs by CCK8 assay Antiproliferative against HLF1 cells measured after 48 hrs by CCK8 assay	[PMID: 36603508]
HSC-T6	IC₅₀	36.23 μM Compound: 6; MP7	Antiproliferative against rat HSC-T6 cells measured after 48 hrs by CCK8 assay Antiproliferative against rat HSC-T6 cells measured after 48 hrs by CCK8 assay	[PMID: 36603508]
IGROV-1	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human IGROV-1 cells measured after 72 hrs by MTT assay Cytotoxicity against human IGROV-1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
LNCaP	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against PTEN-deficient human LNCAP cells after 72 hrs by ATP ViaLight assay Antiproliferative activity against PTEN-deficient human LNCAP cells after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
LS-513	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human LS513 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human LS513 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
MCF7	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human MCF7 cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human MCF7 cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
MCF7	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human MCF7 cells measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
MDA-MB-231	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human MDA-MB-231 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human MDA-MB-231 cells harboring KRAS mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
MDA-MB-453	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human MDA-MB-453 cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human MDA-MB-453 cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
NCI-H1437	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human NCI-H1437 cells after 72 hrs by ATP ViaLight assay Antiproliferative activity against human NCI-H1437 cells after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
NCI-H446	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against PTEN-deficient human NCI-H446 cells after 72 hrs by ATP ViaLight assay Antiproliferative activity against PTEN-deficient human NCI-H446 cells after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
NCI-H69	IC₅₀	13.9 μM Compound: MP-7	Cytotoxicity against human NCI-H69 cells measured after 72 hrs by MTT assay Cytotoxicity against human NCI-H69 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
NCI-H82	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human NCI-H82 cells measured after 72 hrs by MTT assay Cytotoxicity against human NCI-H82 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
NRK-49F	IC₅₀	40.39 μM Compound: 6; MP7	Antiproliferative against rat NRK-49F cells measured after 48 hrs by CCK8 assay Antiproliferative against rat NRK-49F cells measured after 48 hrs by CCK8 assay	[PMID: 36603508]
PC-3	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against PTEN-deficient human PC3 cells after 72 hrs by ATP ViaLight assay Antiproliferative activity against PTEN-deficient human PC3 cells after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
PC-3	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human PC-3 cells measured after 72 hrs by MTT assay Cytotoxicity against human PC-3 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
Rec1	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human REC1 cells measured after 72 hrs by MTT assay Cytotoxicity against human REC1 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
SK-N-MC	IC₅₀	> 30 μM Compound: MP-7	Cytotoxicity against human SK-N-MC cells measured after 72 hrs by MTT assay Cytotoxicity against human SK-N-MC cells measured after 72 hrs by MTT assay	[PMID: 34624821]
T47D	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human T47D cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay Antiproliferative activity against human T47D cells harboring PI3KCA mutant after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
TC-32	IC₅₀	13.9 μM Compound: MP-7	Cytotoxicity against human TC-32 cells measured after 72 hrs by MTT assay Cytotoxicity against human TC-32 cells measured after 72 hrs by MTT assay	[PMID: 34624821]
U-87MG ATCC	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against PTEN-deficient human U87 cells after 72 hrs by ATP ViaLight assay Antiproliferative activity against PTEN-deficient human U87 cells after 72 hrs by ATP ViaLight assay	[PMID: 23448267]
U-87MG ATCC	IC₅₀	> 30 μM Compound: MP7	Antiproliferative activity against human U87MG cells after 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs	[PMID: 27123901]
UMC-11	EC₅₀	> 9 μM Compound: 11	Antiproliferative activity against human UMC11 cells after 72 hrs by ATP ViaLight assay Antiproliferative activity against human UMC11 cells after 72 hrs by ATP ViaLight assay	[PMID: 23448267]

In Vitro

Cell counting of U87MG-derived glioma stem cells (GSCs) confirms that Alisertib and, to a minor extent, MP7 (PDK1 inhibitor) are able to decrease the number of viable cells. When combined together, GSC viability is further reduced with respect to single-treated cells. As observed in U87MG cells, when used at the highest concentrations (i.e., 1.5 μM Alisertib and 2.5 μM MP7), a significant enhancement in the number of dead cells is evidenced. Following 72 h treatment, MP7 alone does not show a significant inhibition of glioblastoma multiforme (GBM) proliferation. MP7 has been shown to have only minimal effects on monolayer cell growth in several cancer cell lines, with IC₅₀ values in the micromolar range^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

516.50

Formula

C₂₈H₂₂F₂N₄O₄

CAS No.

1001409-50-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CN(CC2=CC=C(F)C(F)=C2)C1=O)N[C@H](C3=CC=CC=C3)COC4=CC=C(N5)C(NC5=O)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (193.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9361 mL	9.6805 mL	19.3611 mL
5 mM	0.3872 mL	1.9361 mL	3.8722 mL
10 mM	0.1936 mL	0.9681 mL	1.9361 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.33%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (246 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Daniele S, et al. Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells. ACS Chem Neurosci. 2017 Jan 18;8(1):100-114. [Content Brief]

Cell Assay
^[1]

The human GBM cells (i.e., U87MG, U343MG, or ANGM-CSS) or the respective GSCs are seeded and incubated for the indicated times with the indicated concentrations of SA16 (1 nM to 100 μM), MP7 (2.5 nM, 25 nM, 250 nM and 2.5 μM), or Alisertib. When indicated, cells are treated with MP7 and Alisertib in combination. To verify GSC chemoresistance, U87MG or GSCs are incubated with 50 μM TMZ for 72 h. For the long-term treatment of cells, NSC or complete medium containing drugs is replaced every 3 days. Cell proliferation is determined using the MTS assay: the dehydrogenase activity in active mitochondria reduces MTS to the soluble formazan product, whose absorbance at 490 nm is measured with an automated plate reader. The mean background from each test condition is subtracted, and the data are expressed as the percentage of untreated cells (control). IC₅₀ values are derived from the sigmoid dose-response curve. The percentage of inhibition is calculated as 100% minus the percentage of cell proliferation^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Daniele S, et al. Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells. ACS Chem Neurosci. 2017 Jan 18;8(1):100-114. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9361 mL	9.6805 mL	19.3611 mL	48.4027 mL
	5 mM	0.3872 mL	1.9361 mL	3.8722 mL	9.6805 mL
	10 mM	0.1936 mL	0.9681 mL	1.9361 mL	4.8403 mL
	15 mM	0.1291 mL	0.6454 mL	1.2907 mL	3.2268 mL
	20 mM	0.0968 mL	0.4840 mL	0.9681 mL	2.4201 mL
	25 mM	0.0774 mL	0.3872 mL	0.7744 mL	1.9361 mL
	30 mM	0.0645 mL	0.3227 mL	0.6454 mL	1.6134 mL
	40 mM	0.0484 mL	0.2420 mL	0.4840 mL	1.2101 mL
	50 mM	0.0387 mL	0.1936 mL	0.3872 mL	0.9681 mL
	60 mM	0.0323 mL	0.1613 mL	0.3227 mL	0.8067 mL
	80 mM	0.0242 mL	0.1210 mL	0.2420 mL	0.6050 mL
	100 mM	0.0194 mL	0.0968 mL	0.1936 mL	0.4840 mL

MP7 Related Classifications

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.

Keywords:

MP71001409-50-2PDK1 inhibitorMP 7MP-7PDK-13-Phosphoinositide-dependent protein kinase 1phosphoinositide-dependentkinase-1PDK1Inhibitorinhibitorinhibit

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MP7 (Synonyms: PDK1 inhibitor)

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MP7 Related Antibodies

2 Publications Citing Use of MCE MP7

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MP7 Related Antibodies

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Complete Stock Solution Preparation Table

MP7 Related Classifications

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