PD153035 HCl

Catalog No.S1079

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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PD153035 HCl Chemical Structure

PD153035 HCl Chemical Structure
Molecular Weight: 396.67

Validation & Quality Control

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Product Information

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Product Description

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)
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [2]

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.

Animal Study: [5]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Fry DW, et al. Science. 1994, 265(5175), 1093-1095.

[2] Bos M, et al. Clin Cancer Res. 1997, 3(11), 2099-2106.

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Chemical Information

Download PD153035 HCl SDF
Molecular Weight (MW) 396.67
Formula

C16H14BrN3O2.HCl

CAS No. 183322-45-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms SU-5271 (AG1517) HCl ,ZM 252868 HCl
Solubility (25°C) * In vitro DMSO 0.5 mg/mL (1.26 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride

Customer Product Validation(2)


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Rating
Source J Immunol 2012 188(9), 4581-4589 . PD153035 HCl purchased from Selleck
Method Western blot
Cell Lines RCH-ACV cell
Concentrations 1 μM
Incubation Time
Results Pretreatment with EGFR kinase inhibitors, PD153035 and EKB-569, a potent irreversible inhibitor, abolished the IGF-1- and IL-1β-mediated increase in Bcl-2mRNA levels.

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Rating
Source 2010 Dr. Zhang of Tianjin Medical University. PD153035 HCl purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 0-5 nM
Incubation Time 24 h
Results Increased EGFR, AKT and ERK phosphorylation in T47D cells treated with PD153035 HCl was observed.

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.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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