Almonertinib mesylate is an orally active, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR sensitization and T790M resistance mutations, and also shows strong inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37, 0.29, and 0.21 nM, respectively. The IC50 of T790M/Del19 was 0.37, 0.29 and 0.21 nM, respectively, but the inhibitory effect on wild-type was weaker, with an IC50 of 3.39 nM. It can be used in the research of non-small cell lung cancer.
| Molecular Weight | 621.76 |
| Formula | C31H39N7O5S |
| CAS Number | 2134096-06-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 31.25 mg/mL |
| Storage | 4°C, dry, sealed |
| 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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| Inetetamab
Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab shows antitumor activities when used alone or together with tyrosine kinase inhibitors. |
| 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. |
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