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Product Details

Cabozantinib | Met and VEGFR2 inhibitor

Cabozantinib (849217-68-1) is a novel inhibitor of c-met and VEGFR2 kinase activity, IC50=3.5 nm and 35 pM respectively.1 Inhibits MET-activating kinase domain mutations Y1248H, D1246N or K1262R, IC50=3.8, 11.8 and 14.6 nM respectively. In cellular assays it inhibits the following kinases: MET, VEGF2, KIT, FLT3 and AXL, IC50=7.8, 1.9, 5.0, 7.5 and 42 μM respectively.1 Eliminated approximately 80% of vasculature in spontaneous pancreatic islet tumors over 7 days in a mouse model.2 Clinically useful anticancer agent.3

References/Citations

1) Yakes et al. (2011), Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth; Mol. Cancer Ther., 10 2298
2) You et al. (2011), VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer; Cancer Res., 71 4758
3) Kurzrock et al. (2011), Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor in patients with medullary thyroid cancer; J. Clin. Oncol., 29 2660

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Focus Biomolecules cell signaling supplier, chemical structure of Cabozantinib | MET & VEGFR2 inhibitor | CAS 849217-68-1

Catalog#  10-3231-0005

$70.00
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CAS:
849217-68-1
Catalog Number:
10-3231
Activity:
Met and VEGFR2 inhibitor
Chemical Name:
N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Alternate Names:
XL-184; BMS-907351; Carbozantinib
Molecular Weight:
501.51
Molecular Formula:
C28H24FN3O5
Solubility:
Soluble in DMSO
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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