TP-0903

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Description:IC50: 0.027 μM against AXLAXL and other TAM family members are known to be involved in maintaining the mesenchymal phenotype in cancer cells. Mesenchymal cells have increased invasion and migratory properties, enhanced cell survival in stressed environments, as well as increased resistance to targeted therapies. TP-0903 is a potent anti-cancer agent targeting the AXL receptor tyrosine kinase.In vitro: On the basis of the potency of TP-0903 in biochemical assays, its activity in cell-based studies was evaluated. TP-0903 showed extremely potent activity in cell viability assays against the pancreatic cancer cell line PSN-1. More importantly, TP-0903 was evaluated for its ability to block GAS6-mediated activation of AXL in pancreatic cancer cells. PSN-1 cells were serum-starved and then stimulated with GAS6 in the presence of various concentrations of TP-0903 [1]. In vivo: TP-0903 restores sensitivity to erlotinib in cell-based and preclinical animal models of cancer by reversing the mesenchymal phenotype driving resistance [2]. Clinical trial: Up to now, TP-0903 is still in the preclinical development stage.
    
    [1] Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.
    [2] ToleroPharmaceuticals, Inc–TP-0903. http://www.toleropharmaceuticals.com/TP-0903.html.
- Properties
  - Alternative Name
    
    2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide
    
    CAS Number
    
    1341200-45-0
    
    Molecular Formula
    
    C24H30ClN7O2S
    
    Molecular Weight
    
    516.06
    
    Appearance
    
    A solid
    
    Purity
    
    99.80%
    
    Solubility
    
    ≥25.8 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Rao L, Mak VCY, et al. "p85β regulates autophagic degradation of AXL to activate oncogenic signaling." Nat Commun. 2020;11(1):2291. PMID:32385243

TP-0903

Background

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