Afatinib (BIBW-2992) is an irreversible ErbB family blocker that potently inhibits EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) tyrosine kinases. It exhibits strong inhibitory activity against wild-type EGFR with an IC₅₀ of ~0.5 nM, and mutant forms such as L858R and exon 19 deletions at sub-nanomolar concentrations (IC₅₀ ~0.4–0.9 nM). Afatinib also inhibits HER2 with an IC₅₀ of ~14 nM. It is particularly effective against tumors with EGFR-activating mutations and shows some activity against the T790M resistance mutation, though less potent than osimertinib. In cellular assays, Afatinib blocks EGFR phosphorylation and downstream signaling (e.g., AKT, ERK) and inhibits proliferation of NSCLC cell lines with EGFR mutations (e.g., IC₅₀ ~5–20 nM). Its in vivo efficacy has been demonstrated in xenograft models, showing significant tumor regression at well-tolerated doses.
MedKoo Cat#: 120204
Name: Afatinib dimaleate
CAS#: 850140-73-7 (dimaleate)
Chemical Formula: C32H33ClFN5O11
Exact Mass: 0.0000
Molecular Weight: 718.09
Elemental Analysis: C, 53.52; H, 4.63; Cl, 4.94; F, 2.65; N, 9.75; O, 24.51
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.0 | 79.34 | |
| Water | 32.2 | 44.81 |
The following data is based on the product molecular weight 718.09 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
