Name: IPI-504 (Retaspimycin hydrochloride)
Price: 528.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Retaspimycin hydrochloride (also known as IPI-504), a hydroquinone hydrochloride salt derivative of 17-AAG, is a novel, potent and selective inhibitor of heat shock protein 90(Hsp90) that binds to the amino-terminal ATP/ADP-binding site of Hsp90. As a highly water-soluble version of 17-AAG, IPI-504 (solubility > 200 mg/mL) does not need prior dissolution in organic solvents and hence can be delivered in high concentrations. Once in the systemic circulation, IPI-504 is deprotonated and converted into the free base IPI-504 which is subsequently oxidized to 17-AAG. IPI-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration IC50 values ranging from 10-40 nmol/L and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer.
- Properties
  - Alternative Name
    
    IPI 504, IPI504; [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6,20,22-trihydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16-oxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(22),8,12,14,18,20-hexaen-10-yl] carbamate;hydrochloride
    
    CAS Number
    
    857402-63-2
    
    Molecular Formula
    
    C31H46ClN3O8
    
    Molecular Weight
    
    624.2
    
    Appearance
    
    A solid
    
    Purity
    
    97.56%
    
    Solubility
    
    ≥26.1 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥100 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Katayama K, Noguchi K, et al. "Heat shock protein 90 inhibitors overcome the resistance to Fms-like tyrosine kinase 3 inhibitors in acute myeloid leukemia." Oncotarget. 2018 Sep 28;9(76):34240-34258. PMID:30344940
    2. Dhawan A, Nichol D, et al."Collateral sensitivity networks reveal evolutionary instability and novel treatment strategies in ALK mutated non-small cell lung cancer." Sci Rep. 2017 Apr 27;7(1):1232. PMID:28450729
    3. Debruyne DN, Bhatnagar N, et al. "ALK inhibitor resistance in ALK(F1174L)-driven neuroblastoma is associated with AXL activation and induction of EMT." Oncogene. 2016 Jul 14;35(28):3681-91. PMID:26616860

IPI-504 (Retaspimycin hydrochloride)

IPI-504 (Retaspimycin hydrochloride)

Background

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