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PD153035 HCl EGFR inhibitor

Cat.No.S1079

PD153035 HCl (SU-5271 HCl, AG1517 HCl, ZM 252868 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.
PD153035 HCl EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 396.67

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Quality Control

Batch: S107901 4-Methylpyridine]5 mg/mL]true]DMSO]0.5 mg/mL]false]Water]Insoluble]false Purity: 99.26%
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  • COA
  • NMR
  • HPLC
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  • Datasheet
99.26

Solubility

In vitro
Batch:

4-Methylpyridine : 5 mg/mL

DMSO : 0.5 mg/mL (1.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 396.67 Formula

C16H14BrN3O2.HCl

 Storage (From the date of receipt)
CAS No. 183322-45-4 Download SDF Storage of Stock Solutions

Synonyms SU-5271 (AG1517) HCl ,ZM 252868 HCl Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC.Cl

Mechanism of Action

Targets/IC50/Ki
EGFR
(Cell-free assay)
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. 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. 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. 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.
Kinase Assay
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.
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. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluororuacil in NPCTW04 cells.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22517768/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8824347/
  • [6] https://pubmed.ncbi.nlm.nih.gov/19696185/

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