Art. -Nr.: HY-13686

PQ401

Name: PQ401
Brand: MedChemExpress
SKU: HY-13686
Price: 70.00 USD
Availability: InStock
Rating: 5 (2 reviews)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC₅₀ of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC₅₀, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.

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Reinheit : 99.85%
CAS. Nr.: 196868-63-0
Formel: C₁₈H₁₆ClN₃O₂
Molecular Weight:341.79

Speicherung:

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

PQ401 Chemical Structure

CAS. Nr.: 196868-63-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (5)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IGF-IR; apoptosis^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BJ	EC₅₀	>25 μM Compound: 4{13,1}	Cytotoxicity against human BJ cells after 72 hrs by Cell titer-glo assay Cytotoxicity against human BJ cells after 72 hrs by Cell titer-glo assay	[PMID: 21243104]
HEK293	EC₅₀	>25 μM Compound: 4{13,1}	Cytotoxicity against human HEK293 cells after 72 hrs by Cell titer-glo assay Cytotoxicity against human HEK293 cells after 72 hrs by Cell titer-glo assay	[PMID: 21243104]
HepG2	EC₅₀	>25 μM Compound: 4{13,1}	Cytotoxicity against human HepG2 cells after 72 hrs by Cell titer-glo assay Cytotoxicity against human HepG2 cells after 72 hrs by Cell titer-glo assay	[PMID: 21243104]
MCF7	IC₅₀	12 μM Compound: K00614a, Quinolinyl-urea1	Inhibition of IGF1R autophosphorylation in human MCF7 cells Inhibition of IGF1R autophosphorylation in human MCF7 cells	[PMID: 18077363]
MCF7	IC₅₀	15 μM Compound: K00614a, Quinolinyl-urea1	Growth inhibition of human MCF7 cells Growth inhibition of human MCF7 cells	[PMID: 18077363]
MCF7	IC₅₀	8 μM Compound: K00614a, Quinolinyl-urea1	Inhibition of IGF1R-dependent tumor cell growth in human MCF7 cells Inhibition of IGF1R-dependent tumor cell growth in human MCF7 cells	[PMID: 18077363]
MCF7	IC₅₀	<1 μM Compound: 43	Inhibition of IGF1R autophosphorylation in human MCF7 cells by Western blot analysis Inhibition of IGF1R autophosphorylation in human MCF7 cells by Western blot analysis	[PMID: 19610618]
MCF7	IC₅₀	12 μM Compound: 43	Inhibition of IGF1R autophosphorylation in human MCF7 cells by ELISA Inhibition of IGF1R autophosphorylation in human MCF7 cells by ELISA	[PMID: 19610618]
Raji	EC₅₀	>25 μM Compound: 4{13,1}	Cytotoxicity against human Raji cells after 72 hrs by Cell titer-glo assay Cytotoxicity against human Raji cells after 72 hrs by Cell titer-glo assay	[PMID: 21243104]

In Vitro

PQ401 (1, 5, 10, 25, and 50 μM; 3 days) inhibits proliferation of cultured MCF-7 cells grown in serum or IGF-I in MCF-7 cells^[1].
Twenty-four hours of treatment with 15 μM PQ401 induces caspase-mediated apoptosis^[1].
PQ401 inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC₅₀ <1 μM.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Cell Proliferation Assay^[1]

View Protocol

Cell Line:

Breast cancer cells, MCF-7 cells
Concentration:

1, 5, 10, 25, and 50 μM
Incubation Time:

3 days
Result:

Significantly reduced proliferation (IC₅₀, 8 μM) at concentrations in the range of 1 μM.
Produced a dramatic reduction in cell number from pretreatment levels at concentrations >10 μM.

In Vivo

PQ401 (50 or 100 mg/kg; i.p.; thrice a week) results in a significant dose-dependent reduction in tumor growth over the course of the study. PQ401 reduces the growth rate of MCNeuA cells implanted into mice^[1].

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

Animal Model:

Female mice were MCNeuA tumor cells^[1]
Dosage:

50 or 100 mg/kg
Administration:

Administered i.p. thrice a week; 24 days
Result:

Resulted in a significant dose-dependent reduction in tumor growth. Tumor growth in the animals treated with 100 mg/kg was 20% of that in the vehicle-treated controls. This dosing protocol was well tolerated by the animals.

Chemical Information

CAS. Nr. 196868-63-0
Appearance Solid
Molecular Weight 341.79
Formel C₁₈H₁₆ClN₃O₂
Color White to light yellow
SMILES

O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=C(OC)C=CC(Cl)=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (2)

All WB

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Journal Impact Factor

Nat Cancer

Short-term starvation reduces IGF-1 levels to sensitize lung tumors to PD-1 immune checkpoint blockade. [Abstract]

2020 Jan;1(1):75-85. PMID: 35121837

PQ401 purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2020 Jan;1(1):75-85. [Abstract]

LLC cells cultured under normal or STS-like conditions in the presence of 1 µg/mL rIGF-1, PQ401 (500 ng/mL), their combination or vehicle. GAPDH was used as a control. This experiment was performed once.
EMBO Mol Med

Myeloid p38α signaling promotes intestinal IGF-1 production and inflammation-associated tumorigenesis. [Abstract]

2018 Jul;10(7):e8403. PMID: 29907597

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 14.29 mg/mL (41.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9258 mL

14.6289 mL

29.2577 mL

5 mM

0.5852 mL

2.9258 mL

5.8515 mL

10 mM

0.2926 mL

1.4629 mL

2.9258 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 1.43 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1.43 mg/mL (4.18 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.43 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 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 (14.3 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 8.33 mg/mL (24.37 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 5 mg/mL (14.63 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

All Cell Biology Signal Pathway Related

Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gable KL, Maddux BA, Penaranda C, Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther. 2006 Apr;5(4):1079-86. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9258 mL	14.6289 mL	29.2577 mL	73.1443 mL
	5 mM	0.5852 mL	2.9258 mL	5.8515 mL	14.6289 mL
	10 mM	0.2926 mL	1.4629 mL	2.9258 mL	7.3144 mL
	15 mM	0.1951 mL	0.9753 mL	1.9505 mL	4.8763 mL
	20 mM	0.1463 mL	0.7314 mL	1.4629 mL	3.6572 mL
	25 mM	0.1170 mL	0.5852 mL	1.1703 mL	2.9258 mL
	30 mM	0.0975 mL	0.4876 mL	0.9753 mL	2.4381 mL
	40 mM	0.0731 mL	0.3657 mL	0.7314 mL	1.8286 mL

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PQ401

Publications Citing Use of MedChemExpress (MCE) PQ401