| Name | Falnidamol |
| Description | Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. It displays >1000-fold lower potency against ErbB2 (IC50=3.4 μM) and other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and exhibits anti-cancer activity. |
| Animal Research | Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells
Dosage: 10 mg/kg
Administration: p.o.; daily; 16 days
Result: Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment [2]. |
| In vitro | Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50: 3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM) [1]. Falnidamol demonstrates antiproliferative activity in mitogenic assays performed with KB cells [2]. |
| In vivo | Falnidamol (p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment. Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice. With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 28.8 mg/mL (74.26 mM), Sonication and heating to 60℃ are recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.58 mM), Sonication is recommended.
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| Keywords | Falnidamol | EGFR | BIBX-1382 | BIBX1382 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
