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Icotinib Hydrochloride

EGFR inhibitor,potent and specific CAS# 1204313-51-8

Icotinib Hydrochloride

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Quality Control of Icotinib Hydrochloride

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Chemical structure

Icotinib Hydrochloride

3D structure

Chemical Properties of Icotinib Hydrochloride

Cas No. 1204313-51-8 SDF Download SDF
PubChem ID 44609731 Appearance Powder
Formula C22H22ClN3O4 M.Wt 427.88
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BPI-2009H
Solubility DMSO : 25 mg/mL (58.43 mM; Need ultrasonic)
SMILES C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4.Cl
Standard InChIKey PNNGXMJMUUJHAV-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H21N3O4.ClH/c1-2-16-4-3-5-17(12-16)25-22-18-13-20-21(14-19(18)23-15-24-22)29-11-9-27-7-6-26-8-10-28-20;/h1,3-5,12-15H,6-11H2,(H,23,24,25);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Icotinib Hydrochloride

DescriptionIcotinib Hydrochloride is a potent and specific inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinases with IC50 value of 5 nM.
TargetsEGFR    
IC505 nM     

Protocol

Kinase Assay [1]
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 μCi32P-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 detect radioactivity. Quantification is performed by software[1].

Cell Assay [1]
Cells (1000/well) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37°C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4[1].

Animal Administration [1]
Mice: The effect of three doses of Icotinib (30, 60, and 120 mg/kg/dose p.o. qd) on antitumor activity and survival is determined in mice bearing A431, A549, H460 and HCT8 tumor xenografts. Taxol (30 mg/kg/dose i.p. once a week) is employed in these experiments as a positive control group[1].

References:
[1]. Tan F, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82.

Icotinib Hydrochloride Dilution Calculator

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Icotinib Hydrochloride Molarity Calculator

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Preparing Stock Solutions of Icotinib Hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3371 mL 11.6855 mL 23.371 mL 46.7421 mL 58.4276 mL
5 mM 0.4674 mL 2.3371 mL 4.6742 mL 9.3484 mL 11.6855 mL
10 mM 0.2337 mL 1.1686 mL 2.3371 mL 4.6742 mL 5.8428 mL
50 mM 0.0467 mL 0.2337 mL 0.4674 mL 0.9348 mL 1.1686 mL
100 mM 0.0234 mL 0.1169 mL 0.2337 mL 0.4674 mL 0.5843 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Icotinib Hydrochloride

Icotinib Hydrochloride is a potent and highly selective inhibitor of epidermal growth factor receptor tyrosine kinases (EGFR-TKI) with IC50 value of 5 nM.
EGFR is an oncogenic driver which is expressed on the cell surface of normal cells and cancer cells [1], and patients with somatic mutations, particularly an exon 19 deletion or exon 21 L858R mutation, within the tyrosine kinase domain have activating mutations that lead to unchecked cell proliferation.[2] Overexpression of EGFR caused inappropriate activation of the anti-apoptotic Ras signaling pathway, found in many different types of cancer.[3]
Icotinib is a quinazoline derivative that binds reversibly to the ATP binding site of the EGFR protein, preventing completion of the signal transduction cascade.[4] Icotinib inhibited the intracellular phosphorylation of tyrosine kinase(TK) associated with the epidermal growth factor receptor (EGFR).[5]
Icotinib is indicated for the treatment for EGFR mutation-positive, advanced or metastatic non-small cell lung cancer (NSCLC) as a second-line or third-line treatment, for patients who have failed at least one prior treatment with platinum-based chemotherapy.[6]
References:
1.A Douglas Laird,and Julie M Cherrington. Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. 2003, 12(1): 51-64.
2.Raymond E, Faivre S, Armand JP: Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs. 2000;60 Suppl 1:15-23.
3.Sordella,R. "Gefitinib-Sensitizing EGFR Mutations in Lung Cancer Activate Anti-Apoptotic Pathways". Science ,2004, 305 (5687): 1163-1167.
4.Bulgaru AM. et al. Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase. Expert Rev Anticancer Ther. 2003 Jun;3(3):269-79.
5.Dudek AZ.et al. Skin rash and bronchoalveolar histology correlates with clinical benefit in patients treated with gefitinib as a therapy for previously treated advanced or metastatic non-small cell lung cancer. Lung Cancer. 2006, 51(1):89-96.
6.C Delbaldo, S Faivre, E Raymond. Les inhibiteurs des récepteurs de l’Epidermal Growth Factor (EGF) Epidermal growth factor inhibitors. La Revue de Médecine Interne. 2003,24(6): 372–383.

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References on Icotinib Hydrochloride

[Clinical Observation of Icotinib Hydrochloride for Advanced Non-small Cell Lung Cancer Patients with EGFR Status Identified].[Pubmed:26706949]

Zhongguo Fei Ai Za Zhi. 2015 Dec;18(12):734-9.

BACKGROUND: Icotinib is the first self-developed small molecular drug in China for targeted therapy of lung cancer. Compared to the other two commercially available epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, gefitinib and erlotinib, icotinib is similar to them in chemical structure, mechanism of activity and therapeutic effects. To explore the efficacy and side effects of Icotinib Hydrochloride in the treatment of the advanced non-small cell lung cancer (NSCLC) patients with EGFR mutation and wild-type. METHODS: Patients with advanced NSCLC who were treated with Icotinib Hydrochloride in Beijing Chest Hospital were retrospective analyzed from March 2009 to December 2014. RESULTS: The clinical data of 124 patients (99 with EGFR mutation and 25 with wild type) with advanced NSCLC were enrolled in this study. The patients' overall objective response rate (ORR) was 51.6 % and the disease control rate (DCR) was 79.8%; The patients with EGFR mutation, ORR was 63.6%, DCR was 93.9%. The ORR was 4.0% and the DCR was 24.0% in the wild-type patients. Median progression-free survival (PFS) with icotinib treatment in EGFR mutation patients was 10.5 months and 1.0 month in wild-type patients. The major adverse events were mild skin rash (30.6%) and diarrhea (16.1%). CONCLUSIONS: Monotherapy with Icotinib Hydrochloride is effective and tolerable for the advanced NSCLC EGFR mutation patients.

Icotinib hydrochloride enhances the effect of radiotherapy by affecting DNA repair in colorectal cancer cells.[Pubmed:25572529]

Oncol Rep. 2015 Mar;33(3):1161-70.

The aim of the present study was to explore the efficacy and mechanism of the radiosensitisation of Icotinib Hydrochloride (IH), a novel oral epidermal growth factor receptor-tyrosine kinase activity inhibitor, by evaluating the changes in tumour cell double-strand breaks (DSBs) repair, cell cycle and apoptosis following a combination of IH and radiotherapy (RT) in human colorectal adenocarcinoma cell lines. The HT29 and HCT116 human CRC cell lines were treated with IH and/or radiation. Effects on cell viability and cell cycle progression were measured by MTT, a clonogenic survival assay, and flow cytometry. Immunofluorescent staining and western blot analysis were applied to detect the expression of gamma-H2AX and 53BP1 in the different treatment groups. Finally, the in vivo effect on the growth of CRC xenografts was assessed in athymic nude mice. IH inhibited the proliferation and enhanced the radiosensitivity in HT29 and HCT116 CRC cells lines. IH combined with radiation increased cell cycle arrest in the G2/M phase compared to the other treatments in the HT29 cell line (P<0.05). Similarly, cell cycle arrest occurred in the HCT116 cell line, although this increase did not result in significant differences in the RT group (P>0.05). IH combined with radiation significantly inhibited the expression of gamma-H2AX and 53BP1 based on results of immunofluorescent staining and western blot analysis. In vivo, IH plus radiation significantly inhibited the tumour growth compared to either agent independently. In conclusion, IH significantly increased the radiosensitivity of HT29 and HCT116 cells in vitro and in vivo. Radiation combined with EGFR blockade inhibited tumour proliferation, increased apoptosis, prolonged G2/M arrest and significantly enhanced DNA injury in colorectal cancer. These data support the clinical trials of biologically targeted and conventional therapies in the treatment of cancer.

Efficacy and influence factors of icotinib hydrochloride in treating advanced non-small cell lung cancer.[Pubmed:28165562]

Eur Rev Med Pharmacol Sci. 2017 Jan;21(2):266-274.

OBJECTIVE: To evaluate the efficacy and safety of Icotinib Hydrochloride in the treatment of patients with advanced non-small cell lung cancer (NSCLC) and discuss the influence factors on efficacy. PATIENTS AND METHODS: 120 treatment-experienced patients confirmed by pathology or cytology with stage III B-IV non-small cell lung cancer took Icotinib Hydrochloride and erlotinib orally until the occurrence of disease progression or serious adverse reactions. Then, the efficacy of Icotinib Hydrochloride and the related influence factors were analyzed. RESULTS: In Icotinib Hydrochloride group, the response rate and the disease control rate were 30.00% and 65.00%, and the median progression-free survival time was 179 days (95% CI: 103.21-254.78); in erlotinib group, the response rate and the disease control rate were 25.00% and 56.70%, and the median progression-free survival time was 121 days (95% CI: 95.05-146.94). Moreover, the objective response rate and the disease control rate of second-line therapy were both superior to the third-line and above therapy. The objective response rate of patients with complete response/partial response/stable disease after the first-line therapy was higher than that of patients without response after the first-line therapy (p<0.05), and the significant differences existed in the objective response rate and the disease control rate among mutant group, wild-type group, and unknown group (p<0.05). The response rate and the disease control rate of erythra group were higher than those of non-erythra group (p<0.05). It was showed in the univariate analysis that the progression-free survival was correlated with the smoking status and the epidermal growth factor receptor gene mutations. CONCLUSIONS: The Icotinib Hydrochloride is effective and safe in treating the treatment-experienced patients with advanced NSCLC, especially for patients with sensitive mutations.

Relationship between icotinib hydrochloride exposure and clinical outcome in Chinese patients with advanced non-small cell lung cancer.[Pubmed:26331821]

Cancer. 2015 Sep 1;121 Suppl 17:3146-56.

BACKGROUND: The current study was conducted to explore the relationship between Icotinib Hydrochloride exposure and therapeutic effects in Chinese patients with advanced non-small cell lung cancer (NSCLC) who were treated with Icotinib Hydrochloride. METHODS: A total of 30 patients with NSCLC who were treated with Icotinib Hydrochloride were chosen from a single-center, open-label, phase 1 dose escalation clinical trial. Different doses of Icotinib Hydrochloride were administered orally for 28 consecutive days in different groups until disease progression or unacceptable toxicities occurred. Blood samples were collected during the first treatment cycle (day 1-28) for the pharmacokinetic analysis. Tumor responses were assessed according to the Response Evaluation Criteria in Solid Tumors (RECIST). The plasma concentrations of Icotinib Hydrochloride were assessed by liquid chromatography-mass spectrometry. RESULTS: Thirty patients with a median age of 56 years old (50% of whom were female) were enrolled. For single-dose treatment, the plasma pharmacokinetics demonstrated a median time to maximum concentration of 0.5 to 4 hours and a mean terminal elimination half-life of 6.21+/-3.44 hours at the 150-mg dose and 10.1+/-12.18 hours at the 200-mg dose. For multiple-dose treatment, the last measurable concentration (Clast ) was 708+/-368.67 ng/mL at the 150-mg every 12 hours, 782.73+/-618.18 ng/mL at the 200-mg every 12 hours, and 1162+/-658.44 ng/mL at the 125-mg every 8 hours; the under the concentration curve from time 0 to Clast was 14.5+/-2.43 hour*mg/mL, 13.2+/-2.5 hour*mg/mL, and 12.19+/-2.47 hour*mg/mL, respectively. At the dose of 150 mg every 12 hours, 1 patient with an epidermal growth factor receptor (EGFR) exon 19 deletion achieved a complete response for 10 months; another patient who carried the EGFR exon 19 deletion achieved stable disease for 6 months. Univariate analysis demonstrated that the time to maximum plasma concentration (Tmax ) after a single dose of Icotinib Hydrochloride was significantly correlated with the overall survival (OS) (Spearman correlation coefficient, 0.441; P = .012). The disease control rate was correlated with Tmax after a single dose (Spearman correlation coefficient, 0.518; P = .011). Multivariate analysis demonstrated that the area under the concentration-time curve from 0 to last determination time and the area under the curve from 0 to infinite time after a single dose of Icotinib Hydrochloride were correlated with OS (P = .037 and .042, respectively). The Clast was found to affect progression-free survival (P = .016). Stratification of these patients according to smoking status indicated significant correlation between OS and the area under the concentration-time curve from 0 to last determination time (Spearman correlation coefficient, -0.709; P = .015). CONCLUSIONS: Patients with a longer Tmax and higher exposure might experience longer OS and a higher disease control rate. In addition, the increased Clast might prolong the progressive-free survival of patients. However, the relationships between EGFR mutation, pharmacokinetics, and clinical outcomes require further research.

Description

Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q.

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