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  • Gefitinib (ZD1839)
Gefitinib (ZD1839)的可视化放大

Gefitinib (ZD1839)

An EGFR inhibitor

原价
¥600-762
价格
480-610
Gefitinib (ZD1839)的二维码

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  • 货号: ajci17716
  • CAS: 184475-35-2
  • 别名: 吉非替尼; ZD1839
  • 分子式: C22H24ClFN4O3
  • 分子量: 446.9
  • 纯度: >98%
  • 溶解度: ≥ 22.3mg/mL in DMSO, ≥ 2.48 mg/mL in EtOH with ultrasonic
  • 储存: Store at 2-8°C
  • 库存: 现货

Background

Gefitinib, also known as ZD1839 or Iressa, is a potent and orally-bioavailable small-molecule inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with 50% inhibition concentration IC50 values of 0.033 μM and 0.027 μM in A431 membrane prep and baculovirus lysate respectively. Gefitinib binds to the kinase ATP binding site of EGFR interfering with the binding of adenosine triphosphate, which suppresses the EGFR tyrosine kinase activity and resultant signal transduction of EGFR. Gefitinib exhibits anti-angiogenic activities in a wide range of human tumor types, including head and neck, prostate, breast, ovarian, colon, small-cell lung and non-small-cell lung cancer. Moreover, geftinib has also been found to reduce proliferation, induce cell cycle arrest and increase apoptosis.


吉非替尼,也称为ZD1839或易瑞沙,是一种有效的口服生物可利用的表皮生长因子受体(EGFR)酪氨酸激酶小分子抑制剂,在A431膜制剂和杆状病毒裂解物中的50%抑制浓度IC50值分别为0.033μM和0.027μM。吉非替尼与EGFR的激酶ATP结合位点结合,干扰三磷酸腺苷的结合,三磷酸腺苷抑制EGFR酪氨酸激酶活性和由此产生的EGFR信号转导。吉非替尼在多种人类肿瘤类型中表现出抗血管生成活性,包括头颈部、前列腺、乳腺、卵巢、结肠、小细胞肺和非小细胞肺癌症。此外,格夫替尼还被发现可以减少增殖、诱导细胞周期停滞和增加细胞凋亡。


Reference


[1].M. Ranson and S. Wardell. Gefitinib, a novel, orally administered agent for the treatment of cancer. Journal of Clinical Pharmacy and Therapeutics (2004) 29, 95-103
[2].Joachim Von Pawel. Gefitinib (Iressa, ZD1839): a novel targeted approach for the treatment of solid tumors. Bull Cancer 2004; 91(5): E70-E76

Protocol

Cell experiment: [1]

Cell lines

BT-474 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

1 μM, 24 hours

Applications

A 24-h treatment of BT-474 cells with 1 μM ZD1839 increased the G1 fraction from 74 to 88% and reduced the proportion of cells in S from 15 to 4%. Simultaneous with the accumulation of cells in G1 was complete elimination of both active Akt and MAPK, as measured with phosphospecific antibodies, without changes in the content of total Akt and MAPK. Consistent with the inhibition of Akt activity, phosphorylation of GSK-3β, a target of the Akt kinase, was reduced. Cyclin D1 and Cdk4 were also reduced, whereas protein levels of the Cdk inhibitor p27 were up-regulated.

Animal experiment: [1]

Animal models

Female Balb/C athymic nude mice injected with BT-474 cells

Dosage form

Oral administration, 200 mg/kg/day

Applications

Mice were randomly allocated to either no treatment, ZD1839, Herceptin, or the combination. ZD1839 completely prevented tumor growth but did not induce complete remissions. Herceptin alone induced complete remission in two of seven, whereas the combination resulted in three of eight complete responses. No mice exhibited treatment-related toxicity. Three mice treated with ZD1839 plus Herceptin, in which tumors regressed completely, remained tumor free for > 6 months after discontinuation of therapy and had no detectable tumor at necropsy.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

参考文献:

[1] Moulder S L, Yakes F M, Muthuswamy S K, et al. Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer research, 2001, 61(24): 8887-8895.

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