Icotinib Hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

埃克替尼盐酸盐是埃克替尼的盐酸盐形式，埃克替尼是一种口服的基于喹唑啉的 EGFR 抑制剂，具有潜在的抗肿瘤活性。

Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, has been upregulated in a variety of cancer cell types.

Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation.

Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively.

BPI-2009H

Others

Other Targets

EGFR| EGFR mutants

Cancer

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1204313-51-8

427.88

C22H22ClN3O4

>98% (HPLC)

DMSO : 25 mg/mL. 58.43 mM;

C#Cc1cc(ccc1)Nc1ncnc2cc3OCCOCCOCCOc3cc12.Cl

——

(-20℃)

With Ice Pack

≥ 2 years