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Merck
CN

SML1657

Sigma-Aldrich

吉非替尼

≥98% (HPLC)

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别名:
N-(3-氯-4-氟-苯基)-7-甲氧基-6-(3-吗啉-4-基丙氧基)喹唑啉-4-胺, ZD1839
经验公式(希尔记法):
C22H24ClFN4O3
分子量:
446.90
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 10 mg/mL, clear

储存温度

room temp

SMILES字符串

COC(C=C(N=CN=C1NC2=CC(Cl)=C(F)C=C2)C1=C3)=C3OCCCN4CCOCC4

InChI

1S/C22H24ClFN4O3/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)

InChI key

XGALLCVXEZPNRQ-UHFFFAOYSA-N

基因信息

human ... EGFR(1956)

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应用

吉非替尼已用于:
  • 研究其在子宫内膜癌治疗中的有效应用
  • 细胞增殖、细胞周期和细胞凋亡试验
  • 细胞活力测定和集落形成试验

生化/生理作用

吉非替尼是一种选择性表皮生长因子受体酪氨酸激酶 (EGFR TK) 抑制剂。吉非替尼具有抗肿瘤活性,已被批准用于治疗非小细胞肺癌 (NSCLC)。
吉非替尼对 EGFR 酪氨酸激酶结构域中 ATP(三磷酸腺苷)结合站点的亲和力高于 ATP。因此,已知吉非替尼可抑制子宫内膜癌的进展。

警示用语:

Danger

危险分类

Acute Tox. 4 Oral - Aquatic Chronic 1 - Carc. 2 - Eye Dam. 1 - Repr. 1B - Skin Irrit. 2 - STOT RE 2 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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P M Ellis et al.
Current oncology (Toronto, Ont.), 22(3), e183-e215 (2015-06-20)
This systematic review addresses the use of epidermal growth factor receptor (egfr) inhibitors in three populations of advanced non-small-cell lung cancer (nsclc) patients-unselected, selected, and molecularly selected-in three treatment settings: first line, second line, and maintenance. Ninety-six randomized controlled trials
Silencing of long non-coding RNA MIAT sensitizes lung cancer cells to gefitinib by epigenetically regulating miR-34a.
Fu Y, et al.
Frontiers in Pharmacology, 9, 82-82 (2018)
Xiaozheng Chen et al.
Theranostics, 11(7), 3392-3416 (2021-02-05)
Rationale: Immune checkpoint inhibitors (ICIs) against the PD-1/PD-L1 pathway showed limited success in non-small cell lung cancer (NSCLC) patients, especially in those with activating epidermal growth factor receptor (EGFR) mutations. Elucidation of the mechanisms underlying EGFR-mediated tumor immune escape and
Roy S Herbst et al.
The oncologist, 7 Suppl 4, 9-15 (2002-08-31)
Despite the advent of cisplatin-based combination chemotherapy for advanced non-small cell lung cancer (NSCLC), the prognosis for this patient population remains poor. Novel biologically targeted agents currently in development have the potential for greater efficacy against NSCLC, and possibly less
Brian S Bogdanowicz et al.
Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, 23(3), 203-214 (2016-02-26)
Purpose The approval history, pharmacology, pharmacokinetics, clinical trials, efficacy, dosing recommendations, drug interactions, safety, place in therapy, and economic considerations of gefitinib are reviewed. Summary Lung cancer is one of the most commonly diagnosed cancers and is the leading cause

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