Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. In vivo studies demonstrated that Icotinib exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The compound was well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780).
| Molecular Weight | 427.88 |
| Formula | C22H22ClN3O4 |
| CAS Number | 1204313-51-8 |
| Form | Solid |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related EGFR/HER2 Products |
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| BBT-207
BBT-207 is a reversible, mutant-specific EGFR inhibitor with antitumor activity. |
| VRN-11
VRN-11 is an EGFR C797S inhibitor. |
| TRX-221
TRX-221 is an EGFR C797S inhibitor. |
| TAS-3351
TAS-3351 is an EGFR C797S inhibitor. |
| Larotinib mesylate hydrate
Larotinib mesylate hydrate is a potent, broad-spectrum, orally active tyrosine kinase inhibitor (TKI) that primarily targets EGFR with an IC50 of 0.6 nM. |
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