Icotinib (BPI-2009H) - Moligand™, 10mM in DMSO , Epidermal growth factor receptor erbB1 inhibitor, CAS No.610798-31-7, Epidermal growth factor receptor erbB1 inhibitor
Disponible
SKU
I408103
EGFR/ErbB1 Selective Inhibitors | Activators
Information
Icotinib (BPI-2009H) is a potent and specificEGFRinhibitor withIC50of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
In vitro
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.
Cell Data
cell lines：primary human CLL cells,T cells, NK cells, and epithelial cells
Concentrations：~25 μM
Incubation Time：96 h
Powder Purity:≥99%
Más Información
| CAS | 610798-31-7 |
|---|---|
| Concentración | 10mM in DMSO |
| Sinónimos | [1,4,7,10]Tetraoxacyclododecino[2,3-g]quinazolin-4-amine, N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro- |
| Especificaciones y pureza | Moligand™, 10mM in DMSO |
| Condiciones de almacenamiento de almacenamiento | Store at -80°C |
| Enviado en | Dry ice packs + Cold packs |
| Product Description | Information Icotinib (BPI-2009H) is a potent and specificEGFRinhibitor withIC50of 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. cell lines：primary human CLL cells,T cells, NK cells, and epithelial cells Concentrations：~25 μM Incubation Time：96 h Powder Purity:≥99% |
| Solubilidad | Solubility (25°C) In vitro DMSO: 0.4 mg/mL (1.55 mM); Water: Insoluble; Ethanol: Insoluble; |
| Fórmula molecular | C22H21N3O4 |
Reseñas
Reseñas de cliente
Remind me later