Chemical Property of Cabozantinib Malate
Chemical Property:
- PSA：193.61000
- LogP:4.59340
- Storage Temp.:Sealed in dry,Room Temperature
- Solubility.:DMSO (Slightly), Methanol (Slightly, Heated), Pyridine (Slightly)
- Purity/Quality:
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99%, *data from raw suppliers
Cabozantinib L-Malate Salt *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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Uses
Cabozantinib is a small molecule C-Met modulator. Cabozantinib acts as a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2,
Met, FLT3, Tie2 and Kit, respectively. Cabozantinib shows dose-dependent inhibition of tumor growth and tumor regression, associated with disruption of the tumor vasculature and extensive tumor cell a
poptosis. XL184 (Cabozantinib, BMS-907351) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively. Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
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Clinical Use
Cabozantinib (S)-malate (Cometriq?), which was discovered and developed by Exelixis, gained
approval by the U.S. FDA in November 2012. The drug’s indication is for the treatment of medullary
thyroid cancer (MTC), and is the second drug for this disease after AstraZeneca’s vandetanib
(Caprelsa?). The drug was successfully launched on January 24, 2013. Cabozantinib inhibits
multiple receptor tyrosine kinases including RET, MET, VEGFR-1, -2 and -3, KIT, TRKB, FLT-3,
AXL, and TIE-2. It is currently also undergoing clinical trials for the treatment of prostate, ovarian,
brain, melanoma, breast, non-small cell lung, pancreatic, hepatocellular and kidney cancers.
