中文名称: Pelitinib
英文名称: Pelitinib
CAS No: 257933-82-7
分子式: C24H23ClFN5O2
分子量: 467.92
P10102 Pelitinib ≥98%(HPLC) (psaitong)
外观与性状:
白色至类白色固体
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(5mg/mL 加热)
产品描述:

基本信息

产品编号:P10102

产品名称:Pelitinib

CAS:

257933-82-7

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C24H23ClFN5O2

溶于液体

-80℃

六个月

分子量

467.92

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

13mg/mL (27.78mM)

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

2.1371mL

10.6856mL

21.3712mL

5mM

0.4274mL

2.1371mL

4.2742mL

10mM

0.2137mL

1.0686mL

2.1371mL

 

生物活性

产品描述

一种EGFR(表皮生长因子受体)抑制剂,IC50:38.5nM。

靶点/IC50

EGFR 38.5nM (IC50)

 

体外研究

Pelitini has much greater inhibitory activity against the EGFR kinase than against Src, MEK/ERK, Cdk4, c-Met, Raf and ErbB2,for example, the IC50 for EGFR is 32-fold lower than the IC50 for the closely related ErbB2. Pelitinib results in a dramatic reduction in EGFR phosphorylation but no change in the total amount of EGFR protein. It requires at least 10-fold more drug to equivalently inhibit ErbB2 phosphorylation in similar assays, and EKB-569 does not block phosphorylation of another receptor tyrosine kinase (c-Met) assessed in the same manner[1]. EKB-569 is a potent inhibitor of proliferation in NHEK, A431,and MDA-468 cells (IC50=61, 125, and 260nM, respectively) but not MCF-7 cells (IC50=3600nM). EKB-569 is also a potent inhibitor of EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells (IC50=20-80nM).

 

体内研究

A single oral dose of 10mg/kg EKB-569 inhibits EGFR phosphorylation in A431 xenografts within 60minutes. Twenty-four hours later, EGFR activity is still inhibited by over 50% by this single oral dose. The half-life of EKB-569 in mouse plasma is about 2hours.

 

推荐实验方法(仅供参考)

细胞实验:

 

For experiments using cells in culture, A431 cells or 3T3/c-erbB-2 cells over-expressing c-erbB2 are are treated with various concentrations of EKB-569 for 2.75 h before co-incubation with 100ng/mL EGF (A431 cells) or no growth factor (3T3/c-erbB2 cells) for 0.25h. Cells are ished twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer for 20min on ice, before immunoprecipitation and SDS–PAGE-immunoblotting.

 

动物实验:

 

Mice: For in vivo experiments, athymic nu/nu female mice are implanted subcutaneously with 5×106 A431 tumor cells. When tumors reach a mass of 200-300mg, animals are treated with a single dose of 10mg/kg EKB-569 in pH 2.0 water per gavage.Tumors from control and drug-treated animals are excised and minced into 1-mm pieces for anlysis.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

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稀释公式

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连续稀释计算器方程

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  • 计算结果

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