4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉

中文名称:

4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉

中文同义词:

EGFR抑制剂(PD153035 HYDROCHLORIDE);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;4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉

英文名称:

PD 153035 HYDROCHLORIDE

英文同义词:

4-[(3-BROMOPHENYL)AMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE;PD 153035 HYDROCHLORIDE;PD153035HCl;PD153035;AG1517;PD-153035;AG-1517;ZM 252868;TYRPHOSTIN AG 1517;SU 5271;4-(3-Bromphenylamino)-6,7-bis(methoxy)quinazoline;4-(3-Bromphenylamino)-6,7-dimethylquinazoline;4-Quinazolinamine, N-(3-bromphenyl)-6,7-dimethoxy-;Zinc00600292

CAS号:

153436-54-5

分子式:

C16H14BrN3O2

分子量:

360.21

EINECS号:

相关类别:

信号转导通路激酶抑制剂;小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors;Inhibitor

Mol文件:

153436-54-5.mol

熔点 

189-190 °C

沸点 

472.1±45.0 °C(Predicted)

密度 

1.499±0.06 g/cm3(Predicted)

储存条件 

Keep in dark place,Inert atmosphere,2-8°C

形态

White to off-white solid.

酸度系数(pKa)

5.55±0.30(Predicted)

生物活性

PD153035是一种特定的、有效的EGFR抑制剂，Ki值为5.2 pM。

靶点

Target Value EGFR (Cell-free assay) 5.2 pM(Ki)

Target

Value

EGFR (Cell-free assay)

5.2 pM(Ki)

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.