Name: (R)-Crizotinib
Price: 220.00 USD

- Overview
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    Background
    
    Crizotinib is a potent, ATP-competitive, small-molecule and orally available inhibitor of c-Met kinase with a Ki value of 4 nmol/L[1].
    Crizotinib has shown to inhibit wild-type c-Met phosphorylation with a mean IC50 value of 11 nmol/L in multiple human endothelial and carcinoma cell lines. Crizotinib has been demonstrated to inhibit cell growth and induce apoptosis in human GTL-16 gastric carcinoma cells. Additionally, crizotinib could inhibit cell migration and invasion induced by HGF in human NCI-H441 lung cancer cells. Moreover, crizotinib has revealed to block cell scattering of MDCK [1].
    Crizotinib has been indicated to suppress tumor growth in GTL-16, NCI-H441 NSCLC, Caki-1 RCC, U87MG glioblastoma or PC-3 prostate tumor xenograft mice [1].
    
    [1] Zou HY1, Li Q, Lee JH, Arango ME, McDonnell SR, Yamazaki S, Koudriakova TB, Alton G, Cui JJ, Kung PP, Nambu MD, Los G, Bender SL,Mroczkowski B, Christensen JG. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007 May 1;67(9):4408-17.
- Properties
  - Alternative Name
    
    Crizotinib,PF-2341066, PF02341066, PF 2341066; 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
    
    CAS Number
    
    877399-52-5
    
    Molecular Formula
    
    C21H22Cl2FN5O
    
    Molecular Weight
    
    450.34
    
    Appearance
    
    A solid
    
    Purity
    
    99.79%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥7.51 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lev A, Deihimi S, et al."Preclinical rationale for combination of crizotinib with mitomycin C for the treatment of advanced colorectal cancer." Cancer Biol Ther. 2017 Sep 2;18(9):694-704. PMID:28886275
    2. Huang XX, Xie FF, et al. "Crizotinib synergizes with cisplatin in preclinical models of ovarian cancer." Am J Transl Res. 2017 Apr 15;9(4):1667-1679. PMID:28469773

(R)-Crizotinib

(R)-Crizotinib

Background

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