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PD153035 hydrochloride

Catalog No. T1761   CAS 183322-45-4
Synonyms: ZM 252868 HCl, AG 1517, Tyrphostin AG 1517, SU 5271, PD153035 HCl, ZM 252868

PD153035 hydrochloride (ZM 252868) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PD153035 hydrochloride Chemical Structure
PD153035 hydrochloride, CAS 183322-45-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 62.00
25 mg In stock $ 126.00
50 mg In stock $ 245.00
100 mg In stock $ 417.00
500 mg In stock $ 948.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 100%
Purity: 99.39%
Purity: 99.10%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PD153035 hydrochloride (ZM 252868) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.
Targets&IC50 EGFR:5.2 pM(Ki)
In vitro When administered to HFD-fed mice, PD153035 enhances glucose tolerance, insulin sensitivity, and signaling while reducing subclinical inflammation. In immunodeficient nude mice carrying A431 human epidermoid carcinoma xenografts, PD153035 (80 mg/kg) inhibits the tyrosine kinase activity of the EGF receptor.
In vivo PD153035 exhibits dose-dependent inhibition of nasopharyngeal carcinoma cell lines HONE1 (IC50: 18.6 μM), NPC-TW04 (IC50: 9.8 μM), and NPC-TW01 (IC50: 12.9 μM). It also inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase related to A-431 human squamous epithelial carcinoma (Ki: 5.2 pM, IC50: 29 pM). In Caco-2 colon cancer cells, PD153035 silences COX-2 expression induced by the PAR(2) activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI). Furthermore, PD153035 selectively inhibits EGF-induced tyrosine phosphorylation in Swiss 3T3 fibroblasts and A-431 human squamous epithelial cancer cells (IC50: 15 nM and 14 nM, respectively). When acting on human cancer cell lines overexpressing the EGF receptor, PD153035 suppresses cell growth, including in A431, DU145, Difi, ME180, and MDA-MB-468, with IC50 values of 0.22 μM, 0.4 μM, 0.3 μM, 0.95 μM, and 0.68 μM, respectively.
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.
Cell Research 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)
Synonyms ZM 252868 HCl, AG 1517, Tyrphostin AG 1517, SU 5271, PD153035 HCl, ZM 252868
Molecular Weight 396.67
Formula C16H15BrClN3O2
CAS No. 183322-45-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4 mg/mL (10 mM), with gentle warming

TargetMolReferences and Literature

1. Fry DW, et al. Science. 1994, 265(5175), 1093-1095. 2. Bos M, et al. Clin Cancer Res. 1997, 3(11), 2099-2106. 3. Hsu CH, et al. Oncology. 2005, 68(4-6), 538-547. 4. Hirota CL, et al. Am J Physiol Gastrointest Liver Physiol. 2012 Apr 19. 5. Kunkel MW, et al. Invest New Drugs. 1996, 13(4), 295-302.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library Reprogramming Compound Library Preclinical Compound Library Anti-Lung Cancer Compound Library Kinase Inhibitor Library Angiogenesis related Compound Library Anti-Cancer Compound Library

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Keywords

PD153035 hydrochloride 183322-45-4 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Inhibitor SU-5271 HER1 ZM 252868 HCl AG 1517 PD-153035 ErbB-1 ZM-252868 Tyrphostin AG 1517 PD153035 Hydrochloride PD-153035 Hydrochloride SU 5271 Epidermal growth factor receptor PD153035 PD153035 HCl SU5271 PD 153035 Tyrphostin AG-1517 ZM252868 inhibit PD 153035 Hydrochloride AG1517 PD-153035 hydrochloride AG-1517 ZM 252868 Tyrphostin AG1517 inhibitor

 

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