中文名称: PD153035  一键复制产品信息
英文名称: PD153035
CAS No: 153436-54-5
分子式: C16H14BrN3O2
分子量: 360.2
P10392 PD153035 ≥98%(HPLC) (普西唐-psaitong)
包装规格:
5mg 50mg 250mg in glass bottle
溶解性:
溶于DMSO(30mg/mL 超声)
产品描述:

基本信息

产品编号:P10392

产品名称:PD153035

CAS:

153436-54-5

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C16H14BrN3O2

溶于液体

-80℃

六个月

分子量

360.20

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

6mg/mL (16.65mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.7762mL

13.8808mL

27.7616mL

5mM

0.5552mL

2.7762mL

5.5523mL

10mM

0.2776mL

1.3881mL

2.7762mL

 

生物活性

产品描述

一种有效的EGFR抑制剂,Ki和IC50值分别为6和25pM。

靶点/IC50

EGFR 6pM (Ki)

EGFR 25pM (IC50)

 

体外研究

PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells,with an IC50 of 14 nM[1]. 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 50μM. 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 IC50 is less than 1pM in most cases.

 

体内研究

PD153035 (SU 5271) levels in the plasma and tumor rise to 50 and 22μM within 15minutes following a single i.p. dose of 80mg/kg. While the plasma levels of PD153035 (SU 5271) falls below 1μM 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.

 

推荐实验方法(仅供参考)

细胞实验:

 

Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed.

 

动物实验:

 

Mice: Mice are injected with PD153035 (SU 5271) (80mg/kg) or vehicle and rumors are excised at 20minutes and 180minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD153035 (SU 5271) of the EGF-stimulation.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):