Molecular Formula | C16H14BrN3O2.HCl |
Melting Point | 265°C(lit.) |
Solubility | DMSO: soluble2mg/mL, clear (warmed) |
Appearance | powder |
Color | white to beige |
Storage Condition | Sealed in dry,Room Temperature |
MDL | MFCD01074805 |
Use | PD153035 HCl is a potent, specific EGFR inhibitor with Ki and IC50 of 5.2 pM and 29 pM, respectively; it has little effect on PGDFR, FGFR, CSF-1,InsR and Src. |
In vitro study | PD153035 inhibited A- 431 human squamous cell carcinoma-associated epidermal growth factor receptor tyrosine kinase with a Ki of 5.2 pM and an IC50 of 29 pM. Furthermore, PD 153035 effectively and selectively inhibited EGF-induced tyrosine phosphorylation in Swiss 3T3 fibroblasts and A- 431 human squamous cell carcinoma cells with IC50 of 15 nM and 14 nM, respectively. PD153035 acts on human cancer cell lines that overexpress EGF receptor, including A431, Difi, DU145, MDA-MB-468 and ME180 cells to inhibit growth with IC50 of 0.22 μm and 0.3 μm, respectively, 0.4 M, 0.68 M and 0.95 M. PD153035 inhibited nasopharyngeal carcinoma (NPC) cells, including NPC-TW01, NPC-TW04, and HONE1 cell lines, in a dose-dependent manner with IC50 values of 12.9 μm, 9.8 μm, and 18.6 μm, respectively. Recent studies have shown that PD153035 acts on Caco-2 colon cancer cells, abrogating the COX-2 expression induced by PAR(2) activating peptide 2-furanformyl-LIGRLO-NH(2)(2fLI). PD153035 inhibited A- 431 human squamous cell carcinoma-associated epidermal growth factor receptor tyrosine kinase at K I of 5.2 pM and IC50 of 29 pM. And, PD 153035 effectively and selectively inhibited EGF-induced tyrosine phosphorylation in Swiss 3T3 fibroblasts and A- 431 human squamous cell carcinoma cells with IC50 of 15 nM and 14 nM, respectively. PD153035 acts on human cancer cell lines that overexpress EGF receptor, including A431, Difi, DU145, MDA-MB-468 and ME180 cells to inhibit growth with IC50 of 0.22 μm and 0.3 μm, respectively, 0.4 M, 0.68 M and 0.95 M. PD153035 inhibited nasopharyngeal carcinoma (NPC) cells, including NPC-TW01, NPC-TW04, and HONE1 cell lines, in a dose-dependent manner with IC50 values of 12.9 μm, 9.8 μm, and 18.6 μm, respectively. Recent studies have shown that PD153035 acts on Caco-2 colon cancer cells, abrogating the COX-2 expression induced by PAR(2) activating peptide 2-furanformyl-LIGRLO-NH(2)(2fLI). |
In vivo study | PD153035 inhibited EGF receptor tyrosine kinase activity at a dose of 80 mg/kg in Immunodeficient nude mice bearing A431 human epidermoid carcinoma cell xenografts. PD153035 acts on HFD-fed mice to promote glucose tolerance, insulin sensitivity, and signaling, and to reduce subclinical inflammation. PD153035 at a dose of 80 mg/kg inhibited EGF receptor tyrosine kinase activity in Immunodeficient nude mice bearing transplanted tumor of A431 human epidermoid carcinoma cells. PD153035 acts on HFD-fed mice to promote glucose tolerance, insulin sensitivity, and signaling, and to reduce subclinical inflammation. |
Hazard Symbols | T - Toxic |
Risk Codes | R25 - Toxic if swallowed R37/38 - Irritating to respiratory system and skin. R41 - Risk of serious damage to eyes |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S39 - Wear eye / face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.521 ml | 12.605 ml | 25.21 ml |
5 mM | 0.504 ml | 2.521 ml | 5.042 ml |
10 mM | 0.252 ml | 1.26 ml | 2.521 ml |
5 mM | 0.05 ml | 0.252 ml | 0.504 ml |