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| 25mg |
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Purity: =100%
Icotinib HCl (formerly known as BPI-2009 HCl), the hydrochloride salt of Icotinib and an macrocyclic analog of erlotinib, is an orally bioavailable, potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). Icotinib solely exhibited significant inhibitory activity against EGFR and its mutants when 88 kinases were profiled. In the human epidermoid carcinoma A431 cell line, itotinib inhibits the growth of tumor cells by blocking EGFR-mediated intracellular tyrosine phosphorylation (IC50 = 45 nM). Icotinib showed strong, dose-dependent antitumor effects in nude mice that were bearing different xenografts derived from human tumors, according to in vivo investigations. In mice, the medication was well tolerated at dosages up to 120 mg/kg/day without causing death or appreciable body weight loss while the mice were being treated. Gefitinib was used as an active control in a head-to-head randomized, double-blind phase III trial that was recently completed for patients with advanced non-small cell lung cancer (NSCLC) (Trial registration ID: NCT01040780). According to the data, there was no significant difference between Icotinib and Gefitinib in terms of median progression free survival (PFS), and Icotinib was safer than Gefitinib. In 2011, China approved icotinib for the treatment of lung cancer.
| Targets |
EGFR (IC50 = 5 nM); EGFRL861Q; EGFRL858R/T790M; EGFRL858R; EGFRT790M
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The 2.4 ng/μL EGFR protein and 32 ng/μL Crk are combined in a 25 μL kinase reaction buffer that contains 1 μM cold ATP and 1 μCi32P-γ-ATP for the in vitro kinase assays. A 10-minute ice-based incubation period is used to incubate the mixture at 0, 0.5, 2.5, 12.5, or 62.5 nM of icotinib. A 20-minute curing period is then added. A 10% SDS-PAGE gel is used for electrophoresis to resolve the protein mixture following a 4-minute quench with SDS sample buffer at 100°C. In order to detect radioactivity, the dried gel is subsequently exposed. Software handles quantification[1].
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| Cell Assay |
In RPMI-1640 medium containing 10% FBS, 1000 cells per well are seeded into 96-well plates. The cells are then grown at 37°C in an incubator with 5% CO2. After a day, Icotinib is added to the cells at 0, 0.78, 1.56, 3.125, 6.25, 12.5, or 25 μM for a full day. The calculation of cell proliferation involves deducting the average absorbance value on day 0 from the average absorbance value on day 4 [1].
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| Animal Protocol |
Mice: In mice containing A431, A549, H460, and HCT8 tumor xenografts, the effects of three doses of Icotinib (30, 60, and 120 mg/kg/dose p.o. qd) on antitumor activity and survival are assessed. These studies use taxol (30 mg/kg/dose i.p. once a week) as a positive control group[1].
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| References |
| Molecular Formula |
C22H22CLN3O4
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| Molecular Weight |
427.89
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| Exact Mass |
427.1298839
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| Elemental Analysis |
C, 61.76; H, 5.18; Cl, 8.28; N, 9.82; O, 14.96
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| CAS # |
1204313-51-8
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| Related CAS # |
Icotinib;610798-31-7;Icotinib-d4;1567366-82-8
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| Appearance |
Light yellow solid powder
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| SMILES |
C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4.Cl
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| InChi Key |
PNNGXMJMUUJHAV-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
N-(3-ethynylphenyl)-2,5,8,11-tetraoxa-15,17-diazatricyclo[10.8.0.014,19]icosa-1(12),13,15,17,19-pentaen-18-amine;hydrochloride
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| Synonyms |
BPI-2009; BPI-2009H; BPI2009; BPI 2009; BPI2009H; BPI 2009H; Icotinib; Trade name: Conmana
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3370 mL | 11.6852 mL | 23.3705 mL | |
| 5 mM | 0.4674 mL | 2.3370 mL | 4.6741 mL | |
| 10 mM | 0.2337 mL | 1.1685 mL | 2.3370 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04206072 | Active Recruiting |
Drug: Icotinib Hydrochloride Tablets Drug: D-0316 Capsule |
EGFR Gene Mutation Non-Small Cell Lung Cancer |
Betta Pharmaceuticals Co., Ltd. | December 24, 2019 | Phase 2 Phase 3 |
| NCT01973725 | Active Recruiting |
Drug: Icotinib Hydrochloride | Esophageal Squamous Cell Carcinoma |
Yuhong Li | October 2013 | Phase 2 |
| NCT02574091 | Completed | Drug: 1% icotinib hydrochloride cream Drug: Placebo |
Psoriasis | Betta Pharmaceuticals Co., Ltd. | November 26, 2015 | Phase 1 |
| NCT02934256 | Completed | Drug: Icotinib | Vestibular Schwannoma Neurofibromatosis Type 2 |
Li Peng | July 2016 | Phase 2 |
| NCT01534585 | Completed | Drug: Icotinib Other: Quality of life |
Nasopharyngeal Carcinoma | Taizhou Hospital | February 2012 | Phase 1 Phase 2 |
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