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Icotinib

Cat. No. M1784

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Icotinib Structure
Synonym:

BPI-2009H

Size Price Availability Quantity
10mM*1mL in DMSO USD 90  USD90 In stock
1mg USD 40  USD40 In stock
5mg USD 72  USD72 In stock
10mg USD 105  USD105 In stock
25mg USD 185  USD185 In stock
50mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

Icotinib (BPI-2009H), a highly selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), in two EGFR-mutated lung cancer cell lines compared to A549, a cell line without EGFR mutations. Icotinib blocked EGFR-mediated intracellular tyrosine phosphorylation (IC50 = 45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation.

Protocol (for reference only)
Cell Experiment
Cell lines A431 cell line
Preparation method MTT assay Cells (103/well) were 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 were treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM for 96 h. Cell proliferation was calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4.
Concentrations 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM
Incubation time 96h
Animal Experiment
Animal models mice bearing A431, A549, H460 and HCT8 tumor xenografts
Formulation 0.5% CMCNa
Dosages 30 mg/kg once a week
Administration i.p.
Chemical Information
Molecular Weight 391.4
Formula C22H21N3O4
CAS Number 610798-31-7
Solubility (25°C) DMSO ≥ 72 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Ruan CJ, et al. Eur J Clin Pharmacol. Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers.

[2] Yang G, et al. Oncol Rep. Effects of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in EGFR-mutated non-small cell lung cancer.

[3] Tan F, et al. Lung Cancer. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies.

[4] Wang HP, et al. Chin Med J (Engl). Phase I trial of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in Chinese patients with non-small cell lung cancer.

[5] Zhao Q, et al. Lung Cancer. Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors.

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Keywords: Icotinib, BPI-2009H supplier, EGFR/HER2, inhibitors, activators

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