PD153035 hydrochloride NEW
| Price | $30 | $37 | $75 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PD153035 hydrochloride | CAS No.: 183322-45-4 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PD153035 hydrochloride |
| 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. |
| 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) |
| 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 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4 mg/mL (10 mM), Heating is recommended. |
| Keywords | Inhibitor | SU-5271 | HER1 | PD-153035 | ErbB-1 | PD153035 hydrochloride | ZM-252868 | PD153035 Hydrochloride | PD-153035 Hydrochloride | Epidermal growth factor receptor | PD153035 | SU5271 | PD 153035 | Tyrphostin AG-1517 | ZM252868 | EGFR | inhibit | PD 153035 Hydrochloride | AG1517 | PD-153035 hydrochloride | AG-1517 | Tyrphostin AG1517 |
| Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | JAK-STAT Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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