Name: Cabozantinib malate (XL184)
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Cabozantinib malate is a potent inhibitor of MET andVEGF receptor2 with IC50 values of 1.3nM and 0.035nM [1].Cabozantinib is a pan-tyrosine kinase inhibitor and is developed as an oral treatment of various cancers including MTC, GBM, NSCLC, pancreatic carcinoma, breast and colon cancer. The targets of cabozantinib are MET, VEGFR-2, RET, FLT3, KIT, AXL as well as TEK. In cellular assays, cabozantinib inhibits the phosphorylation of MET, VEGFR2, KIT, FLT3 and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5 and 42μM, respectively [1, 2]. As a pan-tyrosine kinase inhibitor, cabozantinib can affect many biological processes. Cabozantinib inhibits the tubule formation of HMVEC cells with IC50 value of 6.7nM. In B16F10 cells, cabozantinib inhibits HGF-inducedmigration and invasion with IC50 values of 31nM and 9nM, respectively. Moreover, cabozantinib shows anti-proliferation efficacy in a variety of tumors such as SNU-5, Hs746T, MDA-MB-231 and U87MG. It is also reported that the combination of cabozantinib and gefitinib can cause potent inhibition of the gefitinib-resistant HCC827GR6 cell line [1, 2].
    
    [1] Yakes F M, Chen J, Tan J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Molecular cancer therapeutics, 2011, 10(12): 2298-2308.
    [2] Zhang Y, Guessous F, Kofman A, et al. XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC. IDrugs, 2010, 13(2): 112.
- Properties
  - Alternative Name
    
    1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;(2S)-2-hydroxybutanedioic acid
    
    CAS Number
    
    1140909-48-3
    
    Molecular Formula
    
    C32H30FN3O10
    
    Molecular Weight
    
    635.59
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥31.8 mg/mL in DMSO; insoluble in H2O; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mohammad Jafarnejad, Richard J. Sové, et al. "Mechanistically detailed systems biology modeling of the HGF/Met pathway in hepatocellular carcinoma." npj Systems Biology and Applications. 16 August 2019.

Cabozantinib malate (XL184)

Cabozantinib malate (XL184)

Background

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