| Name | Varlitinib |
| Description | Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4. |
| 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[2]. |
| 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. |
| 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 : 31.5 mg/mL (67.46 mM), Sonication and heating to 60℃ are recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.28 mM), Sonication is recommended.
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| Keywords | Varlitinib | HER4 | HER2 | HER1 | ASLAN-001 | ASLAN 001 | ARRY334543 | ARRY 334543 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound 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 Drug Library | Anti-Cancer Active Compound Library |
United States
