CAS NO: | 183322-45-4 |
规格: | ≥98% |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 396.67 |
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Formula | C16H15BrClN3O2 |
CAS No. | 183322-45-4 HCI |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 0.5 mg/mL (1.3 mM) |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
Solubility (In vivo) | 30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL |
Synonyms | SU-5271 HCl , PD 153035; PD-153035; SU 5271 HCl; SU5271 HCl; ZM-252868 HCl; ZM 252868 HCl; ZM252868 HCl; PD153035; PD153035 HCl; PD 153035 HCl; PD-153035 HCl; PD 153035 hydrochloride; PD-153035 hydrochloride; PD153035 hydrochloride; ZM 252868; Tyrphostin AG 1517; AG 1517; ZM-252868; ZM252868; SU-5271, SU 5271; SU5271; |
SMILES Code | N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride |
Chemical NAme | COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC.[H]Cl |
In Vitro | In vitro activity: 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: 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: Cells (A431, Difi, DU145, MDA-MB-468 and ME180) 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. |
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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. |
Animal model | A431 cells are injected into the outbred nude mice. |
Formulation & Dosage | Dissolved in water.; 80 mg/kg; i.p. injection |
References | Science. 1994 Aug 19;265(5175):1093-5; Invest New Drugs. 1996;13(4):295-302. |