中文名 | 盐酸吉非替尼 |
英文名 | Gefitinib hydrochloride |
别名 | 盐酸吉非替尼 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 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 |
英文别名 | Gefitinib Hcl Iressa hydrochloride ZD-1839 hydrochloride Gefitinib hydrochloride Gefitinib hydrochloride salt Gefitinib hydrochloride (ZD-1839 hydrochloride) 4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine hydrochloride |
CAS | 184475-55-6 |
EINECS | 1533716-785-6 |
化学式 | C22H24ClFN4O3.HCl |
分子量 | 483.37 |
InChI | InChI=1/C22H24ClFN4O3.ClH/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15;/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27);1H |
沸点 | 607.7°C at 760 mmHg |
闪点 | 321.3°C |
蒸汽压 | 4.9E-15mmHg at 25°C |
存储条件 | 2-8℃ |
体外研究 | 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. |
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. |
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