Falnidamol

SKU: orb2900173

Description

Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.

Key Properties

• CAS Number: 196612-93-8
• MW: 387.84
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉ClFN₇
• SMILES: CN1CCC(CC1)Nc1ncc2ncnc(Nc3ccc(F)c(Cl)c3)c2n1
• Target: EGFR
• Solubility: In Vitro: DMSO : 31.25 mg/mL (80.57 mM; Ultrasonic (<60°C)

Bioactivity

• In Vivo:
  Falnidamol (BIBX 1382; 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. 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. Animal model: Five-to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells. Dosage: 10 mg/kg (Pharmacokinetic Analysis). Administration: p.o. ; daily; 16 days. Result: The C4h is 2222 nM and the C24h is 244 nM.
• In Vitro:
  Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

EGFR