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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|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||0.5% CMC||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02801435||Not yet recruiting||Psoriasis||Betta Pharmaceuticals Co.,Ltd.|Tigermed Consulting Co., Ltd||July 2016||Phase 1|
|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|
|NCT02737774||Not yet recruiting||Lung Adenocarcinoma||Henan Cancer Hospital||April 2016||Phase 2|
|NCT02744664||Not yet recruiting||Lung Neoplasms||Fuda Cancer Hospital, Guangzhou||April 2016||Phase 4|
|NCT02726568||Recruiting||Non-small Cell Lung Cancer|Brain Metastases||Betta Pharmaceuticals Co.,Ltd.||March 2016||Phase 2|
|NCT02574091||Recruiting||Psoriasis||Betta Pharmaceuticals Co.,Ltd.|Quintiles, Inc.||October 2015||Phase 1|
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