中文名 | PD153035 |
英文名 | PD153035 |
别名 | 化合物PD153035 4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉 N-(3-溴苯基)-6,7-二甲氧基喹唑啉-4-胺 4-[(3-溴苯基)氨基]-6,7-二甲氧基喹唑啉盐酸盐 EGFR抑制剂(PD153035 HYDROCHLORIDE) |
英文别名 | AG1517 AG-1517 SU 5271 PD153035 ZM 252868 PD-153035 PD153035HCl Zinc00600292 TYRPHOSTIN AG 1517 PD 153035 HYDROCHLORIDE 4-(3-Bromphenylamino)-6,7-dimethylquinazoline 4-(3-Bromphenylamino)-6,7-bis(methoxy)quinazoline 4-Quinazolinamine, N-(3-bromphenyl)-6,7-dimethoxy- 4-[(3-BROMOPHENYL)AMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE |
CAS | 153436-54-5 |
化学式 | C16H14BrN3O2 |
分子量 | 360.21 |
密度 | 1.499±0.06 g/cm3(Predicted) |
熔点 | 189-190 °C |
沸点 | 472.1±45.0 °C(Predicted) |
溶解度 | 溶于DMSO (高达5 mg/ml)。 |
酸度系数 | 5.55±0.30(Predicted) |
存储条件 | Keep in dark place,Inert atmosphere,2-8°C |
稳定性 | 从提供的购买之日起稳定1年。在DMSO中的溶液可以在-20 ° 储存长达3个月。 |
外观 | 白色至灰白色固体。 |
颜色 | White or off-white |
体外研究 | PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC 50 of 14 nM. PD153035 (SU 5271) has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD153035 (SU 5271) rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD153035 (SU 5271) causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC 50 is less than 1 pM in most cases. |
体内研究 | PD153035 (SU 5271) levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD153035 (SU 5271) falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.776 ml | 13.881 ml | 27.762 ml |
5 mM | 0.555 ml | 2.776 ml | 5.552 ml |
10 mM | 0.278 ml | 1.388 ml | 2.776 ml |
5 mM | 0.056 ml | 0.278 ml | 0.555 ml |
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