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Postion:Product Catalog >Biochemical Engineering>Inhibitors>protein tyrosine kinase>Varlitinib
Varlitinib
  • Varlitinib

Varlitinib NEW

Price $30 $58 $103
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Varlitinib CAS No.: 845272-21-1
Purity: 99.7% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameVarlitinib
DescriptionVarlitinib (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 vitroIn 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 vivoVarlitinib 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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 31.5 mg/mL (67.5 mM), Sonication and heating to 60℃ are recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsVarlitinib | ARRY 334543 | ARRY334543 | ASLAN-001 | ASLAN 001
Inhibitors RelatedTucatinib | AG-1478 | (S)-Afatinib | Mollugin | Tannic acid | Afatinib Dimaleate | Neratinib | Cisapride | Pyrotinib dimaleate | AG1557 | Sarizotan 2HCl | VU 0240551
Related Compound LibrariesBioactive Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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