Varlitinib

SKU: orb1685624

Description

Varlitinib (ASLAN001) is a reversible pan-EGFR inhibitor with potent activity against HER1 (IC50=7 nM), HER2 (IC50=2 nM), and HER4 (IC50=4 nM). It is a research tool used in vitro and in vivo for studying EGFR-driven cancers, including biliary tract and gastric malignancies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 845272-21-1
• MW: 466.94
• Purity: 99.70%
• Formula: C₂₂H₁₉ClN₆O₂S
• SMILES: C[C@@H]1COC(Nc2ccc3ncnc(Nc4ccc(OCc5nccs5)c(Cl)c4)c3c2)=N1
• Target: HER,EGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.28 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:31.5 mg/mL (67.46 mM)

Bioactivity

• Target IC50:
  ErbB2:2 nM|ERB1:7 nM|HER4:4 nM
• In Vivo:
  Varlitinib treatment effectively suppresses tumor growth, achieving complete tumor regression at a dosage of 100 mg/kg administered twice daily. Within five days of treatment, Varlitinib significantly inhibits the phosphorylation of key signaling molecules including HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal protein, 4EBP1, Cdk-2, Cdc-2, and retinoblastoma. This inhibition is accompanied by a marked decrease in survivin levels and an increase in Caspase 3 cleavage products, indicating enhanced apoptosis. Additionally, in murine xenograft models, Varlitinib (ARRY-334543) shows substantial, dose-dependent tumor growth inhibition in A431-derived tumors when given orally at doses of 25, 50, and 100 mg/kg, twice a day for 21 days.
• In Vitro:
  In cell-based assays involving tumor cells with over-expression of EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) effectively inhibits substrate phosphorylation and demonstrates high selectivity for EGFR/ErbB-2 without significant activity against a panel of 104 other kinases.

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

ARRY 334543, ARRY334543, ARRY-334543, ASLAN001, ASLAN-001, ASLAN 001, HER1, HER2, HER4, Varlitinib

Compound Identifiers

PubChem CID

42642648