PQ401

Name: PQ401
Brand: MedChemExpress
SKU: HY-13686
Rating: 5.0 (3 reviews)

Cat. No.: HY-13686 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

PQ401 Chemical Structure

CAS No. : 196868-63-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE PQ401

: PQ401 purchased from MedChemExpress. Usage Cited in: Nature Cancer. 75-85 (2020).; 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.

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Biological Activity
Purity & Documentation
References
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Description

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	< 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.

Cell Proliferation Assay^[1]

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.

Molecular Weight

341.79

Formula

C₁₈H₁₆ClN₃O₂

CAS No.

196868-63-0

Appearance

Solid

Color

White to light yellow

SMILES

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

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 : 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 : 1 mg/mL (2.93 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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: ≥ 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.
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% (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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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

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: 99.85%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (261 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.9258 mL	14.6289 mL	29.2577 mL	73.1443 mL
DMSO	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

Keywords:

PQ401196868-63-0PQ 401PQ-401IGF-1RApoptosisInsulin-like growth factor-1 receptorautophosphorylationMCF-7cellsbreastcancercaspaseapoptosisInhibitorinhibitorinhibit

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PQ401

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PQ401 Related Antibodies

2 Publications Citing Use of MCE PQ401

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Complete Stock Solution Preparation Table

PQ401 Related Classifications

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