Gefitinib hydrochloride

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CAS NO:

184475-55-6

盐酸吉非替尼
ZD-1839 hydrochloride

Gefitinib hydrochloride (ZD1839 hydrochloride) 是一种有效，选择性和口服活性的EGFR酪氨酸激酶抑制剂，IC₅₀为 33 nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC₅₀为 54 nM)，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。

生物活性

Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally activeEGFRtyrosine kinaseinhibitor with anIC₅₀of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC₅₀of 54 nM) and that blocks EGF-stimulatedEGFRautophosphorylation in tumor cells. Gefitinib hydrochloride also inducesautophagy. Gefitinib hydrochloride has antitumour activity^[1]^[2].

IC₅₀& Target^[1]

EGFR

体外研究
(In Vitro)

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^[1]. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC₅₀of 20 nM^[2]. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC₅₀of 2 μM^[3].

体内研究
(In Vivo)

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^[3]. 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^[4].

Clinical Trial

分子量

483.36

性状

Solid

Formula

C₂₂H₂₅Cl₂FN₄O₃

CAS 号

184475-55-6

中文名称

盐酸吉非替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 6.25 mg/mL(12.93 mM;Need ultrasonic)

DMSO : 0.227 mg/mL(0.47 mM;Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.0689 mL	10.3443 mL	20.6885 mL
5 mM	0.4138 mL	2.0689 mL	4.1377 mL
10 mM	0.2069 mL	1.0344 mL	2.0689 mL

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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。