4-(3-氯-4-氟苯基氨基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉盐酸盐
中文名称 | 4-(3-氯-4-氟苯基氨基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉盐酸盐 |
---|---|
中文同义词 | 盐酸吉非替尼;4-(3-氯-4-氟苯基氨基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉盐酸盐;吉非替尼盐酸盐;吉非替尼原料药;EGFR酪氨酸激酶抑制剂;GEFITINIB盐酸盐;化合物 T1181L;盐酸吉非替尼(吉非替尼杂质50) |
英文名称 | 4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride |
英文同义词 | 4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride;Gefitinib hydrochloride;Gefitinib Hcl;ZD-1839 hydrochloride;Iressa hydrochloride;Gefitinib hydrochloride (ZD-1839 hydrochloride);Gefitinib hydrochloride salt |
CAS号 | 184475-55-6 |
分子式 | C22H25Cl2FN4O3 |
分子量 | 483.37 |
EINECS号 | 1533716-785-6 |
相关类别 | 抗肿瘤药物;医药中间体;细胞生物学试剂 |
Mol文件 | 184475-55-6.mol |
结构式 |
4-(3-氯-4-氟苯基氨基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉盐酸盐 性质
储存条件 | Store at -20°C |
---|---|
溶解度 | 不溶于乙醇; ≥4.28 mg/mL,在 H2O 中,温和加热和超声波;温和加热下 DMSO 中≥6.9 mg/mL |
形态 | 粉末 |
Target | Value |
EGFR
(Cell-free assay) | 15.5 nM |
EGFR (858R/T790M)
(Cell-free assay) | 823.3 nM |
Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine 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 (1-2 mM) 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 IC 50 of 20 nM. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC 50 of 2 μM.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/01/25 | HY-50895A | 4-(3-氯-4-氟苯基氨基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉盐酸盐 Gefitinib hydrochloride | 184475-55-6 | 100mg | 550元 |
2024/01/25 | HY-50895A | 4-(3-氯-4-氟苯基氨基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉盐酸盐 Gefitinib hydrochloride | 184475-55-6 | 10mM * 1mLin Water | 605元 |