Falnidamol (BIBX 1382) is an orally active, reversible, and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. In preclinical studies, BIBX 1382 exhibited potent inhibition of EGFR autophosphorylation with an IC₅₀ of ~10–20 nM in EGFR-overexpressing cell lines such as A431. It effectively blocked downstream signaling pathways, including ERK and AKT, and inhibited proliferation of EGFR-dependent tumor cells with GI₅₀ values in the low nanomolar range. In xenograft models, BIBX 1382 demonstrated significant antitumor activity, especially in tumors with wild-type EGFR and high receptor expression.
MedKoo Cat#: 561225
Name: Falnidamol HCl
CAS#: 1216920-18-1 (2HCl)
Chemical Formula: C18H21Cl3FN7
Exact Mass: 0.0000
Molecular Weight: 460.76
Elemental Analysis: C, 46.92; H, 4.59; Cl, 23.08; F, 4.12; N, 21.28
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.4 | 42.08 | |
| Water | 19.4 | 42.08 |
The following data is based on the product molecular weight 460.76 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 |
