Catalog No.S2922 Synonyms: BPI-2009H
Molecular Weight(MW): 391.42
Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
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B. Effect of Icotinib treatment on the subcellular localization of ABCG2 in NCI-H460/MX20 cell. ABCG2 staining is shown in green. DAPI (blue) counterstains the nuclei. C. Effect of Icotinib on the ATPase activity of ABCG2: The BeFx-sensitive specific ATPase activity of ABCG2 was determined in the presence of 0-5 μM of Icotinib as described in supplemental methods. The activity in the absence of Icotinib (basal activity) was considered to be 100%, and % -fold stimulation ± S.D. (Y-axis) was plotted as a function of indicated concentrations of Icotinib (X-axis). D. Effect of Icotinib on the photolabeling of ABCG2 with [125I]-IAAP: Crude membranes from ABCG2 expressing MCF7-FLV1000 cells were photo-crosslinked with [125I]-IAAP in the presence and absence of 0-50 μM of Icotinib as described in supplemental methods. [125I]-IAAP incorporated in ABCG2 band was quantified using ImageQuant software and plotted as % [125I]-IAAP incorporated ± S.D. (Y-axis) as a function of varying concentration of Icotinib (X-axis). The upper panel shows a representative autoradiogram from three independent experiments and the arrow represents the ABCG2 band photo-crosslinked with [125I]-IAAP.
Oncotarget, 2015, 5(12):4529-42.. Icotinib purchased from Selleck.
Purity & Quality Control
Choose Selective EGFR Inhibitors
|Description||Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).|
Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR. 
|In vivo||Icotinib shows an antitumor effect in different types of xenografts. Icotinib inhibits tumor growth at a rate of 51.5%, 31.0% and 67.4% in the A431, A549 and H460 xenografts at a dose of 120 mg/kg, respectively. |
Biochemical kinase assays:In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi 32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30 °C for 20 min. After quenching with SDS sample buffer at 100 °C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to the PhosphorImager to detect radioactivity. Quantification is performed by ImageQuant software. In this methodology the radioactive signal inversely correlates with kinase activity.
|In vitro||DMSO||78 mg/mL (199.27 mM)|
|Ethanol||7 mg/mL (17.88 mM)|
|In vivo||Add solvents individually and in order:
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02961270||Recruiting||Non-small Cell Lung Cancer||Chinese Academy of Medical Sciences||November 2016||Phase 2|
|NCT02960607||Recruiting||Carcinoma, Non-Small-Cell Lung||Chinese Academy of Medical Sciences||November 2016||Phase 2|
|NCT02934256||Recruiting||Vestibular Schwannoma|Neurofibromatosis Type 2||Li Peng|Betta Pharmaceuticals Co.,Ltd.|Beijing Tiantan Hospital||July 2016||Phase 2|
|NCT02801435||Recruiting||Psoriasis||Betta Pharmaceuticals Co.,Ltd.|Tigermed Consulting Co., Ltd||July 2016||Phase 1|
|NCT02883543||Active, not recruiting||Non-small Cell Lung Cancer||Daping Hospital and the Research Institute of Surgery of the Third Military Medical University||June 2016||Phase 3|
|NCT02820116||Recruiting||Non-small Cell Lung Cancer(NSCLC)||Beijing Haidian Hospital|Peking University Peoples Hospital|307 Hospital of PLA|309th Hospital of Chinese Peoples Liberation Army||May 2016||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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