Home Protein Tyrosine Kinase IGF-1R inhibitor PQ 401 For research use only.

PQ 401

PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.

PQ 401 Chemical Structure

PQ 401 Chemical Structure

CAS: 196868-63-0

Selleck's PQ 401 has been cited by 3 Publications

3 Customer Reviews

Purity & Quality Control

Batch: S800301 DMSO] 32 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.99%
99.99

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Signaling Pathway

IGF-1R Signaling Pathways

IGF-1R Signaling Pathway

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Biological Activity

Description PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
Targets
IGF-1R [1]
<1 μM
In vitro
In vitro PQ 401 is an IGF-1R inhibitor and inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1μM. PQ 401 significantly reduced proliferation of MCF-7 cells with IC50 of 8 μM. PQ 401 also inhibits growth of MCNeuA cells with IC50 of 15 μM. PQ 401 inhibits the IGF-I-mediated antiapoptotic pathway in MCF-7 cells. PQ 401 increases caspase-mediated apoptotic activity in MCF-7 cells. [1]
Kinase Assay IGF-IR Peptide Autophosphorylation
One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/− varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80μMEGTA, 0.25% 2-mercaptoethanol, 80μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20).
Cell Research Cell lines MCF-7, MCNeuA
Concentrations ~50 μM
Incubation Time 3 days
Method The inhibitory effects of diaryl urea on breast cancer cell growth are determined using a CyQuant cell proliferation assay kit. MCF-7 or MCNeuA cells are plated in 96-well plates (5 × 103 per well) in phenol red-free DMEM supplemented with 10% FCS. One plate isprepared for each harvest day. Cells are allowed to adhere overnight and are then treated with various concentrations of diaryl urea or DMSO as a vehicle control. Microplate cultures are harvested on days 0, 1, 2, and 3 by inverting the microplate onto paper towels with gentle blotting to remove growth medium without disrupting adherent cells. Each plate iskept at −80 ℃ until the end of the experiment (day 3) when all of the plates are thawed and assayed together. After thawing, 200 μL of CyQuant GR solution are added to each well and the plates are incubated in the dark for 2 to 5 minutes. Fluorescence ismeasured with a SpectraMax Gemini XS fluorescence microplate reader with 480-nm excitation and 520-nm emission. Proliferation index iscalculated as the percent of nucleotide content versus control cells at day 0.
In Vivo
In vivo PQ 401 (50 mg/Kg, 100 mg/Kg) significantly inhibits MCNeuA tumor growth in a dose-dependent manner. [1]
Animal Research Animal Models FVB/N-TgN(MMTVneu)202 mouse injected with MCNeuA cells.
Dosages 50 or 100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 341.79 Formula

C18H16ClN3O2
CAS No. 196868-63-0 SDF Download PQ 401 SDF
Smiles CC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 32 mg/mL ( (93.62 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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