Name: CH5424802
Price: 236.00 USD

- Overview
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    Background
    
    CH5424802 is a potent and selective ALK inhibitor.
    Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers. .
    In vitro: In cell free assays the IC50 of CH5424802 for enzyme activity of ALK was 1.9 nM; the dissociation constant (KD) value for ALK in an ATP-competitive manner was 2.4 nM. The inhibitory activity for two hot spot-activating mutations (F1174L and R1275Q) in neuroblastoma was comparable to that for wildtype ALK [1].
    In vivo: In the NCI-H2228 model, oral administration of CH5424802 resulted in dose-dependent tumor growth inhibition (ED50 = 0.46 mg/kg) and tumor regression. Moreover, treatment of 20 mg/kg CH5424802 showed rapid tumor regression and tumor regrowth did not occur throughout the 4-week drug-free period [2].
    Clinical trial: No clinical data are available currently.
    
    [1] Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.
- Properties
  - Alternative Name
    
    9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
    
    CAS Number
    
    1256580-46-7
    
    Molecular Formula
    
    C30H34N4O2
    
    Molecular Weight
    
    482.62
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥2.72 mg/mL in EtOH with gentle warming; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CH5424802

CH5424802

Background

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