PD153035 HCl

Catalog No.S1079 Synonyms: SU-5271 (AG1517) HCl ,ZM 252868 HCl

PD153035 HCl Chemical Structure

Molecular Weight(MW): 396.67

PD153035 HCl is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.

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3 Customer Reviews

  • B. Increased of cell migration induced by EGF is inhibited by a selective ATP competitive inhibitor of EGFR (PD153035). Histograms showing HCT-116 cell migration with or without treatment by EGF +/− PD153035. Results are expressed as mean ± SEM. ***p<0.001, sample significantly different from control (N=3, n=7, Kruskal-Wallis test).

    Oncotarget, 2016, 7(24):36168-36184.. PD153035 HCl purchased from Selleck.

    IGF-1 and IL-1β mediated induction of Bcl-2 expression involves EGFR.   (A)  Bcl-2 mRNA levels in AALEBs treated with IGF-1 or IL-1β in the presence or absence of two EGFR tyrosine kinase inhibitors, EKB-569 (1 μM) or PD153035 (1 μM).  

    J Immunol 2012 188(9), 4581-4589 . PD153035 HCl purchased from Selleck.

  • T47D cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of  PD153035 for 24 hours.

     

     

    2010 Dr. Zhang of Tianjin Medical University. PD153035 HCl purchased from Selleck.

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Biological Activity

Description PD153035 HCl is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
Targets
EGFR [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
5.2 pM(Ki) 5.2 pM(Ki)
In vitro

PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively. [1] PD153035 shows growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines including A431, Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22 μM, 0.3μM, 0.4 μM, 0.68 μM and 0.95 μM, respectively. [2] PD153035 induces a dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC) cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of 12.9 μM, 9.8 μM and 18.6μM, respectively. [3] A recent study shows that PD153035 abolishes COX-2 expression induced by the PAR(2)-activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI) in Caco-2 colon cancer cells. [4]

In vivo In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity. [5] PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. [6] Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluororuacil in NPCTW04 cells. [3]

Protocol

Kinase Assay:[1]
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Inhibition of EGF receptor tyrosine kinase :

Enzyme reactions are performed in a total volume of 0.1 mL containing 25 mM Hepes (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 50 μM sodium vanadate, 0.5 to 1.0 ng of enzyme (which also contains enough EGF to make the final concentrations 2 μg/mL), 10 μM ATP containing 1 μCi of [32P]ATP, varying concentrations of PD153035, and 200 μM of a substrate peptide based on a portion of phospholipase C-γl having the sequence Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction is initiated by the addition of ATP. After 10 minutes at room temperature, the reaction is terminated by addition of 2 mL of 75 mM phosphoric acid, and the solution is passed through a 2.5-cm phosphocellulose filter disk that binds the peptide. The filter is washed five times with 75 mM phosphoric acid and placed in a vial with 5 mL of scintillation fluid. The uninhibited control activity produces approximately 100,000 cpm.
Cell Research:[2]
+ Expand
  • Cell lines: A431, Difi, DU145, MDA-MB-468 and ME180
  • Concentrations: 0-3 μM
  • Incubation Time: 72 hours
  • Method: Cells are seeded in sixwell plates. The next day, cells are changed to medium containing 0.5% FBS for 18 hours, and then PD153035 is added at various concentrations to the cultures. After 72 hours of treatment, cells are washed once with PBS, harvested with 0.1% human trypsin-l mM EDTA in PBS, and counted with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.
    (Only for Reference)
Animal Research:[5]
+ Expand
  • Animal Models: A431 cells are injected into the outbred nude mice.
  • Formulation: PD153035 is dissolved in water.
  • Dosages: ≤80 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.5 mg/mL (1.26 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 396.67
Formula

C16H14BrN3O2.HCl

CAS No. 183322-45-4
Storage powder
in solvent
Synonyms SU-5271 (AG1517) HCl ,ZM 252868 HCl

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID