Erlotinib metabolite M12 - CAS 183321-84-8
Molecular Formula:
C20H19N3O4
Molecular Weight:
365.389
COA:
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Description:
A metabolite of Erlotinib. Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity.
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Synonyms:
4-[(3-Ethynylphenyl)amino]-6,7-bis(2-hydroxyethoxy)quinazoline; 2-(4-(3-Ethynylanilino)-7-(2-hydroxyethoxy)quinazolin-6-yl)oxyethanol; 2-[4-(3-ethynylanilino)-7-(2-hydroxyethoxy)quinazolin-6-yl]oxyethanol
MSDS:
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InChIKey:
YWSAEKIQJPQSDJ-UHFFFAOYSA-N
InChI:
InChI=1S/C20H19N3O4/c1-2-14-4-3-5-15(10-14)23-20-16-11-18(26-8-6-24)19(27-9-7-25)12-17(16)21-13-22-20/h1,3-5,10-13,24-25H,6-9H2,(H,21,22,23)
Canonical SMILES:
C#CC1=CC(=CC=C1)NC2=NC=NC3=CC(=C(C=C32)OCCO)OCCO
1.[Clinical Observation of Icotinib Hydrochloride for Advanced Non-small Cell Lung Cancer Patients with EGFR Status Identified].
Li X1, Qin N1, Wang J1, Yang X1, Zhang X1, Lv J1, Wu Y1, Zhang H1, Nong J1, Zhang Q1, Zhang S1. Zhongguo Fei Ai Za Zhi. 2015 Dec 20;18(12):734-9. doi: 10.3779/j.issn.1009-3419.2015.12.04.
in English, Chinese背景与目的 盐酸埃克替尼(icotinib hydrochloride)是我国第一个具有自主知识产权的小分子靶向抗癌新药,与吉非替尼和厄洛替尼相比,在化学结构、分子作用机理、疗效等方面相似。本研究观察盐酸埃克替尼治疗表皮生长因子受体突变状态明确的晚期非小细胞肺癌(non-small cell lung cancer, NSCLC)的疗效和毒副反应。方法 回顾性分析2009年3月-2014年12月间北京胸科医院收治的晚期NSCLC患者,表皮生长因子受体(epidermal growth factor receptor, EGFR)突变状态已知,均口服盐酸埃克替尼治疗,评价其疗效和毒副反应。结果 124例组织学证实的晚期NSCLC患者,其中EGFR突变型99例,野生型25例。全组客观有效率(objective response rate, ORR)为51.6%,疾病控制率(disease control rate, DCR)为79.8%。突变型和野生型患者的ORR:63.6% vs 4.0%,DCR:93.9% vs 24.0%,两者均有统计学差异(P<0.000,1)。突变型和野生型患者的无进展生存期(progression-free survival, PFS)(分别为10.5个月和1.0个月)(P<0.000,1)。治疗相关的毒副反应主要为皮疹38例(30.6%),腹泻20例(16.1%)。结论 盐酸埃克替尼治疗EGFR突变的晚期NSCLC疗效肯定,耐受性好。.
2.[Gefitinib therapy in advanced non-small cell lung cancer in patients with EGFR mutations: cost-effectiveness analysis].
Protsenko SA, Rudakova AV. Vopr Onkol. 2015;61(4):676-80.
Therapy for advanced non-small cell lung cancer (NSCLC) is very complex clinical problem. The optimal choice of therapy demands not only the analysis of data on clinical effectiveness, but also an assessment of cost-effectiveness of the applied drugs. The current options for first- or second/third-line of lung cancer treatment are tirosine kinase inhibitors (TKI)--gefitinib, erlotinib and afatinib. According to the received results TKI first-line therapy for NSCLC in patients with EGFR mutations is not only clinically effective but also is economically acceptable from a position of the Russian budgetary health care. TKI second-line therapy for NSCLC patients who fail first-line therapy also provides improvement of the quality of life and prolonged time to progression. Comparable clinical effectiveness and safety of erlotinib and gefitinib in patients with EGFR mutations allows making drug choice on the basis of regional price characteristics.
3.Epidermal growth factor receptor-inhibition (EGFR-I) in the treatment of neuropathic pain.
Kersten C1, Cameron MG2, Laird B3, Mjåland S2. Br J Anaesth. 2015 Nov;115(5):761-7. doi: 10.1093/bja/aev326.
BACKGROUND: Neurobiological work has demonstrated that expression of mitogen-activated protein kinases (MAPK) is upregulated on neurones and glial cells after nerve damage. Furthermore, the epidermal growth factor receptor (EGFR) has been identified as having a key role in this process and subsequent interruption of this using EGFR-Inhibitors (EGFR-I), may improve neuropathic pain. The aim of this report was to explore if EGFR-I attenuated neuropathic pain in humans.
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CAS 183321-84-8 Erlotinib metabolite M12

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