中文名称: 盐酸吉非替尼
英文名称: Gefitinib hydrochloride
CAS No: 184475-55-6
分子式: C22H25Cl2FN4O3
分子量: 483.36
G10683 盐酸吉非替尼 ≥98% (psaitong)
包装规格:
100mg 500mg 1g 5g in glass bottle
产品描述:

基本信息

产品编号:G10683

产品名称:Gefitinib hydrochloride

CAS:

184475-55-6

 

储存条件

粉末

-20℃

三年

分子式:

C22H25Cl2FN4O3

溶于液体

-80℃

两年

分子量

483.36

 

 

化学名: 

N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine;hydrochloride

 

Solubility (25°C)

 

体外

DMSO

3 mg/mL (6.2mM)

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

2.069mL

10.3443mL

20.6885mL

5mM

0.4138mL

2.0689mL

4.1377mL

 

生物活性

产品描述

一种有效,选择性和口服活性的 EGFR 酪氨酸激酶抑制剂,IC50 为 33nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50 为 54nM),并阻断 EGF 刺激的肿瘤细胞中 EGFR 自磷酸化。Gefitinib hydrochloride 还可诱导细胞自噬 (autophagy),并具有抗肿瘤活性。

靶点/IC50

EGFR 
(Cell-free assay)

EGFR (858R/T790M)
(Cell-free assay)

15.5nM

 

 

体外研究

hosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM. Gefitinib leads to an inhibition of CALU 3 and GLC82 cell proliferation, with an IC50 of 2μM. .

 

体内研究

Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice

bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts. In irradiated rats, Gefitinib

treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression,

while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation.

 

推荐实验方法(仅供参考)

细胞实验:

 

Cancer cells are seeded in 96-well plates and are treated with different doses of Gefitinib (0.01-20μM), Metformin or both for 72 hours. Cell proliferation is measured with the MTT assay. The IC50 values are determined by interpolation from the doseresponse curves. Results represent the median of 3 separate experiments each conducted in quadruplicate. The results of the combined treatment are analyzed according to the method of Chou and Talalay by using the CalcuSyn software program.

 

动物实验:

 

Ice Four- to 6-week old female balb/c athymic (nu+/nu+) mice are acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that has been resuspended in 200μL of Matrigel. When established tumors of approximately 75 mm3 in diameter are detected, mice are left untreated or treated with oral administrations of metformin (200mg/mL metformin diluted in drinking water and present throughout the experiment), gefitinib (150mg/kg daily orally by gavage), or both for the indicated time periods. Each treatment group consists of 10 mice. Tumor volume is measured using the formula π/6×larger diameter×(smaller diameter)2 . Rats The rats are randomly assigned to 1 of 4 experimental groups: 1) the unirradiated rats treated with oral administration of vehicle (0.1% Tween 80) once daily;(2) the unirradiated rats treated with oral administration of gefitinib (50 mg/kg/day) once daily;(3) the irradiated rats treated with oral administration of vehicle once daily; 4) the irradiated rats treated with oral administration of gefitinib once daily. Each experimental group comprised 5-6 rats and all treatments are delivered for 14days.

 

 

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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    *
    *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):