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Gefitinib hydrochloride

Gefitinib hydrochloride

盐酸吉非替尼

Catalog No.

A3433

EGFR有效的抑制剂

组合的产品项目
规格	价格	库存	数量
100mg	￥ 1,136.00	现货

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背景
化学属性
试验操作
质量控制

背景

EGFR（表皮生长因子受体）是分子量为170，000的具有一个外部结合域和一个胞内酪氨酸激酶域的跨膜糖蛋白。Gefitinib (ZD-1839，Iressa)是一种表皮生长因子受体选择性激酶抑制剂。

体外: 在所有癌症细胞系中，吉非替尼以剂量依赖的方式抑制在软琼脂上的集落形成。然而，高剂量治疗导致细胞凋亡增加2-4倍。毒性药物与吉非替尼处理癌细胞剂量依赖性抑制细胞生长。联合治疗显著增强单药治疗引起的凋亡性细胞死亡[1]。

体内:在人GEO结肠癌异种移植裸鼠中，吉非替尼治疗可逆性地和剂量依赖地抑制肿瘤生长，GEO肿瘤在治疗结束时恢复了对照组的增长速度[1]。

临床试验:250毫克剂量的吉非替尼作为分散制备饮料或鼻胃管实现系统性接触吉非替尼时，与作为药片给药效果一致。没有证据表明耐受性与

符合实现管理作为一个整体平板电脑。在健康患者中没有证据表明耐受性与给药路线相关[2]。

参考文献：
[1] Ciardiello F, Caputo R, Bianco R, Damiano V, Pomatico G, De Placido S, Bianco AR, Tortora G. Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clin Cancer Res. 2000;6(5):2053-63.
[2] Cantarini MV, McFarquhar T, Smith RP, Bailey C, Marshall AL. Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers. Clin Ther. 2004;26(10):1630-6.

化学属性

Storage	Store at -20°C
M.Wt	483.36
Cas No.	184475-55-6
Formula	C₂₂H₂₅Cl₂FN₄O₃
Synonyms	Iressa hydrochloride;ZD 1839 hydrochloride;ZD-1839 hydrochloride;ZD1839 hydrochloride
Solubility	insoluble in EtOH; ≥4.28 mg/mL in H2O with gentle warming and ultrasonic; ≥6.9 mg/mL in DMSO with gentle warming
Chemical Name	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine;hydrochloride
SDF	Download SDF
Canonical SMILES	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl
运输条件	蓝冰运输或根据您的需求运输。
一般建议	不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

试验操作

Cell experiment:[1]
Cell lines	Human ovarian (OVCAR-3), breast (ZR-75–1, MCF-10A ras), and colon cancer (GEO) cells that coexpress EGFR and TGF-α
Reaction Conditions	0.01 ~ 50 μM gefitinib for 5 d incubationn
Applications	Gefitinib (0.01 ~ 50 μM; 5 d) inhibited colony formation in soft agar in a dose-dependent manner in all cancer cell lines. The antiproliferative effect was mainly cytostatic. However, treatment with higher doses (0.05, 0.1 or 1 μM; 3 d) resulted in a 2 ~ 4-fold increase in apoptosis.
Animal experiment:[1]
Animal models	Nude mice bearing established human GEO colon cancer xenografts
Dosage form	1.25, 2.5 or 5 mg/dose Administered intraperitoneally on days 1 ~ 5 of each week for 4 weeks
Applications	Gefitinib treatment produced a dose-dependent inhibition of GEO tumor growth that was almost completely suppressed in mice treated with the 5 mg of daily dose. Gefitinib treatment was generally well tolerated by mice with no signs of acute or delayed toxicity. Although GEO tumor growth was only delayed, mouse survival duration was significantly increased in the gefitinib (5 mg/dose)-treated group.
Note	The technical data provided above is for reference only.
	References: 1. Ciardiello F, Caputo R, Bianco R, et al. Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clinical Cancer Research, 2000, 6(5): 2053-2063.