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Icotinib

Cat. No. M1784
Icotinib Structure
Synonym:

BPI-2009H

Size Price Availability Quantity
10mg USD 305 In stock
25mg USD 550 In stock
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Quality Control
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 391.4
Formula C22H21N3O4
CAS Number 610798-31-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers.
Ruan CJ, et al. Eur J Clin Pharmacol. 2012 May 15. PMID: 22585284.

Effects of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in EGFR-mutated non-small cell lung cancer.
Yang G, et al. Oncol Rep. 2012 Jun;27(6):2066-72. PMID: 22446631.

Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies.
Tan F, et al. Lung Cancer. 2012 May;76(2):177-82. PMID: 22112293.

Phase I trial of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in Chinese patients with non-small cell lung cancer.
Wang HP, et al. Chin Med J (Engl). 2011 Jul 5;124(13):1933. PMID: 22088449.

Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors.
Zhao Q, et al. Lung Cancer. 2011 Aug;73(2):195-202. PMID: 21144613.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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