Falnidamol

SKU: orb1679006

Description

Falnidamol (BIBX 1382) is a pyrimido-pyrimidine-based, orally bioavailable small molecule that potently and selectively inhibits EGFR tyrosine kinase (IC50=3 nM). It exhibits over 1000-fold selectivity against ErbB2 and is used in cancer research for its anti-proliferative effects in both cellular and animal models of EGFR-driven tumors.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 196612-93-8
• MW: 387.84
• Purity: 98.82% (May vary between batches)
• Formula: C₁₈H₁₉ClFN₇
• SMILES: CN1CCC(CC1)Nc1ncc2ncnc(Nc3ccc(F)c(Cl)c3)c2n1
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.58 mM);DMSO:28.8 mg/mL (74.26 mM)

Bioactivity

• Target IC50:
  ErbB2:3.4 μM|EGFR:3 nM
• 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 .
• 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) . Falnidamol demonstrates antiproliferative activity in mitogenic assays performed with KB cells .
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EGFR, Falnidamol, BIBX 1382, BIBX1382, BIBX-1382

Compound Identifiers

PubChem CID

6918508